tag:blogger.com,1999:blog-65665743783619747112024-02-06T23:30:13.873-04:00Molecules and MaterialsShaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.comBlogger59125tag:blogger.com,1999:blog-6566574378361974711.post-86488324308312178512020-07-09T11:02:00.001-03:002020-07-09T11:08:36.671-03:00Foldscope: A microscope for everyone<div dir="ltr" style="text-align: left;" trbidi="on">
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Imagine a bookmark-sized device that is made of paper and can be attached to a phone to view the microscopic world-this is the Foldscope. This foldable micro-optics–embedded device costs less than $2 and has the capability to magnify an object more than 140 times its original size, with a resolution of 2 microns. This resolution is enough to view bacteria, parasites, plant structures, blood cells, etc.</div>
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Prof. Manu Prakash and Dr. Jim Cybulski at Stanford University, USA, are the co-developers of the Foldscope. Working together at Prakash Labs, they have provided a clear path forward for viewing the microscopic world, well beyond the 500-year-old conventional microscope technology. Utilizing basic principles of optics and origami, the researchers came up with the design for the Foldscope. Three essential components-an illuminator, a sample holder, and an optical viewing device are created by folding paper and then pieced together. Adding in a combination of lenses yields a user-friendly device that can be used without the requirement of external power sources. The tool, which is available for everyone, has already reached a million users spanning across ~145 countries. Apart from its popular use in science education, the Foldscope is also considered a radical new technology that might improve public health, especially in the developing world. At present, there are several investigations into its diagnostic applications in order to provide cheaper alternatives to current methods reported in scientific journals. However, real-world applications are yet to take off. </div>
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It is also amazing how the Twitter community is posting interesting microscopic pictures and real-time videos under tags like #foldscope. These allow easy access to the beautiful and intricate scientific nature of microorganisms. Access to such information also raises curiosity among students who don’t have accessibility to traditional microscopes. The Department of Biotechnology (DBT), India and Prakash Labs have signed a memorandum to bring the Foldscope to India. Rafikh Shaikh, a Foldscope Fellow at Tata Institute of Social Sciences (TISS) in Mumbai is a prolific user and student trainer of the Foldscope. He claims, “Children are curious by nature, they explore the world around them and construct knowledge. Frugal tools like Foldscope (a paper microscope) help children in their inside school and out of school explorations. As Foldscope is small and can fit in a pocket, children can carry it anywhere. Unlike a traditional microscope, you don't have to carry a sample to the lab, you can observe it on the spot. Each observation answers some questions and raises more questions feeding into a child's curiosity-driven explorations. We have seen school children using Foldscope and online community websites to understand their surroundings and also connecting it with the school science”.</div>
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Due to the inexpensive nature of and easy access to this useful technique, there could be many possibilities of scientific applications the Foldscope can offer. During a recent interview with Eric Topol of Medscape, Prof. Manu Prakash described his vision for the Foldscope, termed Octopi (Open Configurable high-Throughput Platform for Infectious diseases).“One of the big things I am excited about that is not yet public is that we will be announcing the 100 Octopi Program. One of the challenges with AI is what data you train with. Real-time data coming from the field, from the context, is always a challenge because many times the hardware has switched, so you trained on one hardware, and then suddenly it's a different hardware,” he stated. With the Octopi program, Prof. Prakash aims for high-speed detection of diseases such as malaria.</div>
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The Foldscope is on the right track to revolutionize the 500-year-old technology. Not only does this invention provide a visual treat of the microscopic world that is not accessible to the naked eye, but it also offers diagnostic use in healthcare applications. The Foldscope is definitely a scientific innovation for everyone.</div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com3tag:blogger.com,1999:blog-6566574378361974711.post-45006619867485264382018-12-24T00:24:00.002-04:002021-03-18T08:20:51.733-03:00Artificial polymerases<div dir="ltr" style="text-align: left;" trbidi="on">
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</div><div style="text-align: justify;"><span data-preserver-spaces="true" style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;">The development of synthetic catalysts that has parallel enzymatic efficiency in terms of rate and turnover is still a challenge in chemistry. The <i>de novo</i> design of a biochemical system in a molecular matrix is fascinating and challenging for future synthetic catalysis. </span><a class="editor-rtfLink" href="https://pubs.rsc.org/en/content/articlelanding/2018/cc/c8cc05804k/unauth#!divAbstract" style="color: #4a6ee0; margin-bottom: 0pt; margin-top: 0pt; text-align: start;" target="_blank"><span data-preserver-spaces="true" style="margin-bottom: 0pt; margin-top: 0pt;">We recently used</span></a><span data-preserver-spaces="true" style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;"> a non-covalent interaction approach to create nano-sized artificial enzymes for the size, shape, stereo, and enantio-selective synthesis of small molecules and polymers.</span></div><div style="text-align: justify;">
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<a href="https://pubs.rsc.org/en/Image/Get?imageInfo.ImageType=GA&imageInfo.ImageIdentifier.ManuscriptID=C8CC05804K" style="margin-left: 1em; margin-right: 1em;"><img alt="Graphical abstract: Directional threading of a chiral porphyrin cage compound onto viologen guests" border="0" src="https://pubs.rsc.org/en/Image/Get?imageInfo.ImageType=GA&imageInfo.ImageIdentifier.ManuscriptID=C8CC05804K" title="Graphical abstract" /></a> </div>
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<a href="https://pubs.acs.org/doi/abs/10.1021/acs.orglett.8b01055">These biomimetic</a> systems not only provide fresh insight into elucidating the catalytic mechanism of natural enzymes but also demonstrate the underlying principles in structure-based catalysis. The newly discovered chiral catalytic host can move along polymer chains in a single direction like natural enzymes, polymerases, and ribosomes. Such synthetic catalytic machines could be used for the synthesis of sequence-controlled polymers as well as for data storage.</div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com1tag:blogger.com,1999:blog-6566574378361974711.post-2789413270798420562014-10-13T15:10:00.000-03:002014-10-20T15:45:22.636-03:00Supramolecular Chemistry in Drug Discovery<div dir="ltr" style="text-align: left;" trbidi="on">
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<span style="color: #444444; font-family: Arial, Helvetica, sans-serif;"><b><span style="background-color: white; text-align: start;">Contributing writer</span><span style="line-height: 18px; text-align: left;"> Lily Bryant</span></b></span></div>
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<span style="color: #444444; font-family: Arial, Helvetica, sans-serif;">Supramolecular chemistry has important medical applications, as it aids the development of new drug therapies by helping researchers to understand how medications <a href="http://syntheticorganic.blogspot.co.uk/2013/01/modulators-of-proteinprotein.html">interact at the target binding sites</a> in the body. This area of chemistry has also aided the development of binding drugs that are able to alter the target substance and its properties, so the substrate is unable to reach its action site or trigger the usual biological response. Examples of this are the phosphate binding drug sevelamer hydrochloride, which is used to manage raised phosphate levels in advanced cases of chronic kidney disease, and the selective binding agent sugammadex, which reverses neuromuscular block brought on by vecuronium and rocuronium <a href="http://www.sciencedirect.com/science/article/pii/S0168365911002422">during anesthesia</a>. However, supramolecular chemistry is also important for the development of drug delivery systems, which offer encapsulation and targeted release.</span></div>
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<b><span style="color: #444444; font-family: Arial, Helvetica, sans-serif;"><a href="http://en.wikipedia.org/wiki/Peptoid_nanosheet">Peptoid nanosheets</a><o:p></o:p></span></b></div>
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<span style="color: #444444; font-family: Arial, Helvetica, sans-serif;">Researchers from Lawrence Berkeley National Laboratory have recently made a development that will hopefully pave the way to more effective and safer drug delivery systems. These systems can help to reduce the unwanted <a href="http://www.clevelandclinic.org/Myeloma/Pain%20Management.htm">side-effects associated drug therapies</a>, which are sometimes severe enough to discourage patients from accepting medication or mean that they have to abandon treatment. As with opiate based painkillers, the untargeted nature of their actions means that <a href="http://www.drugtreatment.com/topics/choose-a-top-inpatient-krokodil-treatment-rehab/">some drugs may even lead to addiction</a>. While <a href="http://professional.medtronic.com/pt/neuro/idd/edu/patient-selection/#.VDlI-xby-f4">intrathecal delivery of painkillers</a> can help those people struggling with chronic pain that is difficult to control, it isn’t without its risks and more precise targeting of drugs with the aid of molecular delivery systems could offer more successful results without the adverse effects.</span></div>
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<span style="color: #444444; font-family: Arial, Helvetica, sans-serif;">The team which previously
developed peptoid nanosheets that come together where air and water meet have
<a href="http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4169914/">now created peptoid</a> nanosheets that come together where oil and water meet.
If you are not familiar with the concept of a peptoid nanosheet, this is a
synthetic 2D protein structure, which typically has a thickness of just three
nanometers, making it one of the thinnest organic 2D crystalline materials
available. Just like natural proteins, peptoids are able to fold and curve into
specific shapes, enabling them to complete precise functions. As it is possible
to customize the peptoids from which they are formed, this makes the properties
of these nanosheets flexible, meaning that they are a good candidate in the
area of drug delivery. Additionally, the very large surface area of peptoid
nanosheets makes them ideal for sensing and recognition, which is again vital
for drug delivery. Another useful property for these applications is
their hydrophobic core, which excludes water molecules, meaning that peptoid
nanosheets have the potential to carry hydrophobic cargos, as demonstrated by
research published in <i><a href="http://pubs.acs.org/doi/abs/10.1021/nn403899y">ACS Nano</a></i>. Finally, peptoids are
not as sensitive to chemical or metabolic changes as proteins, so they are less
likely than natural proteins to break down, which is advantageous when using
them within the body.</span></div>
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<span style="font-family: Arial, Helvetica, sans-serif;"><span style="color: #444444;">The latest findings, which were published in the September edition of the <a href="http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4169914/">Proceedings of theNational Academy of Sciences USA,</a> show how it is possible for these specific and highly organized peptoid sheets to form at a water-oil interface. Spectroscopic measurements confirm that the monolayers are extremely well ordered and that it is the electrostatic action between charged molecules on the peptoid that allow the formation of this orderly structure at the surface of oil and water. The ability to create these nanosheets using oil instead of air creates new possibilities for their production6. It would also allow the development of libraries of various functionalized nanosheets and allow screening for peptoid nanosheets that have the same molecular recognition as specific proteins, which would aid future drug discoveries. While the production of peptoid nanosheets with drugs in their interior is still some way off, these findings open up the possibility of extending the complexity and functions of 2D nanomaterials, which can only aid the development of drug delivery systems.</span></span><br />
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<span style="font-family: Arial, Helvetica, sans-serif;"><b style="line-height: 18px;"><span style="color: #444444;">About Lily Bryant</span></b></span></div>
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<span style="color: #444444; font-family: Arial, Helvetica, sans-serif;">Lily Bryant is a writer working with one of only two licensed online pharmacies in the US. She is strongly interested in promoting and creating content aimed at relevant readers as part of her role in ethical healthcare business. She believes that it is important that we play a strong role in leading society towards a healthier lifestyle through the promotion of exercise and healthy diet rather than an early adoption of drug treatment.</span></div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com1tag:blogger.com,1999:blog-6566574378361974711.post-80517373841494507022014-09-23T16:03:00.002-03:002021-03-21T08:40:12.059-03:00Old wisdom new tools<div dir="ltr" trbidi="on">
Some of the shapes depicted in ancient artifacts that were invisible to the human eye came into view with the advent of 20th-century tools. Some being nano and microstructures. These tools also help chemists to see the formation of chemical bonds in real-time. </div><div dir="ltr" trbidi="on"><div style="text-align: justify;">The rapid development of modern nano-technological tools such as the <a href="https://www.blogger.com/#">Atomic Force Microscope (AFM)</a>, <a href="https://www.blogger.com/#">Scanning Tunnelling Microscope</a> (STM), and Laser Scanning<a href="https://www.blogger.com/#"> Confocal Microscope</a> (LSCM) allow scientists to invent, explore and validate old scientific discoveries. From the perspective of scientists involved with chemistry, it helps to manipulate atoms and molecules precisely for the fabrication of macroscale products as well as to look at the real-time covalent bond formation in a single molecule. Observing chemical reactions by force microscopy at sub-molecular resolution has been reported by de <a href="https://www.blogger.com/#">Oteyza </a><a href="https://www.blogger.com/#">et al</a>. They reported the atomically resolved imaging of a complex molecule as it undergoes a chemical reaction on a metal surface.</div><div style="text-align: justify;"><br /></div><div class="separator" style="clear: both; text-align: center;">
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<div style="text-align: justify;">In addition to the normal covalent bond formation, very recently <a href="https://www.blogger.com/#">Wilson Ho et.al.,</a> revealed the image of hydrogen bonding in porphyrin molecules using chemically modified STM tip, enlightening us with the rapid advance in this field. These developments will have a huge impact in nanoscience especially in the field of single molecular electronics and bottom-up fabrications. This new evolution of molecular nanotechnology will bring chemists, physicists, engineers, and biologists together.</div><div style="text-align: justify;"><br /></div><div class="separator" style="clear: both; text-align: center;">
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<div style="text-align: justify;">How practical is it to prove old theories with modern, technologically advanced tools? Is it really possible? However, if it is indeed possible, would it be a landmark achievement that would push chemistry into a new era, in the coming years? Let me exemplify. <a href="https://www.blogger.com/#">Mayan blue</a> is a bright blue pigment that had been used by Mayans about 2000 years ago to paint murals. The distinct feature about these murals is that the Mayan-blue has withstood the wrath of weather over centuries, and refuse to fade even to this day. on the On the other hand, even the most advanced of paints of today, tend to wear off after a couple of years of harsh weather and negligent maintenance. This is a phenomenon that has baffled scientists for several years. They were able to gain some insight into this in the recent past with the help of modern nanotechnological tools. The Mayan dye is based on Indigo dye, which is trapped in a porous fame work of clay called <a href="https://www.blogger.com/#">palygorskite</a>. The silicate hull forms a protective layer around the dye molecules. This prevents the dye pigments from directly interacting with the forces of nature and other interferences such as organic solvents, acid, and alkali treatment, etc.</div><div class="MsoNormal" style="line-height: normal; margin-bottom: 0cm; text-align: justify; text-indent: 36pt; text-justify: inter-ideograph;"><span style="font-family: "times new roman"; font-size: 12pt; text-indent: 36pt;"><br /></span></div>
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<div class="MsoNormal" style="text-align: justify;">It is the Mayan's ingenuity at developing the pigments for Mayan blue that has set them eons beyond outreach. Reverse engineering could help us understand its structure and shed some light into the properties of advanced hybrid materials. Maybe, the day is not far off when we are able to decode this chemical phenomenon and come up with commercial paints that will last forever.</div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com1tag:blogger.com,1999:blog-6566574378361974711.post-62919580710236317152013-10-05T12:20:00.008-03:002021-03-21T08:43:05.916-03:00Cooperative Catalysis<div dir="ltr" style="text-align: left;" trbidi="on">
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<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhZ6IzG-rZEopsU_gzxzYcmvvlKhodjeZECThYW8z1JT6kA_GBKY-tv6QyjXfnxGSbn9hYldBe06h2lN5h164_bb2On8GTwc3tfEm8-FdV0xaT-qMbMOWO4nJLJsYCbGkCnllVpCig_8ZrE/s1600/New+Picture+2.png" style="clear: left; float: left; margin-bottom: 1em; margin-right: 1em; text-align: justify;"><img border="0" height="125" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhZ6IzG-rZEopsU_gzxzYcmvvlKhodjeZECThYW8z1JT6kA_GBKY-tv6QyjXfnxGSbn9hYldBe06h2lN5h164_bb2On8GTwc3tfEm8-FdV0xaT-qMbMOWO4nJLJsYCbGkCnllVpCig_8ZrE/s320/New+Picture+2.png" width="320" /></a></div>
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<span face="arial, helvetica, sans-serif">Cooperative catalysis occurs when the synergic catalytic effect of at least two different entities acts together, increasing the rate of a chemical reaction beyond what is possible when either of the two entities is used independently. The idea of “Cooperative Catalysis” has inspired synthetic chemists to create artificial dual activation catalysts. Such a Cooperative Catalytic pathway is often used in enzymatic catalysis. Enzymes are continue to be a source of inspiration for (designing and) developing new catalytic reactions that are high in efficiency & selectivity and minimal waste.</span></div>
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<span face="arial, helvetica, sans-serif"><a href="http://en.wikipedia.org/wiki/Urease">Urease</a> is a dinuclear metalloenzyme which catalyzes the hydrolysis of urea into carbon-di-oxide and ammonia. The dimeric nickel center of this enzyme is (the active site) responsible for cooperative catalysis. Urea co-ordinates with one Ni-center, thus activate the electrophile (act as Lewis Acid), whereas water coordinates with the second Ni. It is thus acidified and can be deprotonated by histidine to generate hydroxide as a nucleophile (generate nucleophile), which is, now in close to the electrophile, and, can attack in an intramolecular fashion.</span></div>
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<span face="arial, helvetica, sans-serif">A similar cooperative catalytic activity with Bronsted and Lewis acidities can be generated by simultaneous incorporation of multiple elements in the silica framework is quite interesting and holds promises of unprecedented catalytic performances.</span></div>
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<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEh12vcs4Odqk1JlVdVULhoMchn9eQ0yg9NvLBGrPf_p9qDJOBSp2L0ObbFBDIq5qAT9ouaZkzJ8-845L9mgZDEHyOzYCFdfMjjzG_R-B1qD1nMNFpYkNn7q4aIWK2JYCZijcIpgviB_6dnR/s1600/New+Picture.png" style="clear: right; float: right; margin-bottom: 1em; margin-left: 1em;"><img border="0" height="183" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEh12vcs4Odqk1JlVdVULhoMchn9eQ0yg9NvLBGrPf_p9qDJOBSp2L0ObbFBDIq5qAT9ouaZkzJ8-845L9mgZDEHyOzYCFdfMjjzG_R-B1qD1nMNFpYkNn7q4aIWK2JYCZijcIpgviB_6dnR/s200/New+Picture.png" width="200" /></a><span face="arial, helvetica, sans-serif"><a href="http://onlinelibrary.wiley.com/doi/10.1002/cctc.201200332/abstract">We recently prepared</a> a similar natural mimic, a bimetallic nano-porous catalytic system, which would be able to perform cooperative catalysis for the selective synthesis of ortho-prenylated phenols and 2,2-dimethyl chroman, starting from phenol and allylic alcohol. Prenylated phenols are widely distributed in nature and are known to be an important structural unit of pharmaceutical compounds. Similarly, 2,2-dimethylchroman derivatives also exhibit broad range of interesting physiological properties, we are able to synthesis the important structural motif by using the new cooperative catalytic systems.</span></div>
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<span face="arial, helvetica, sans-serif">The amount of aluminum present in the framework dictates the acidity of the catalyst, and by fine-tuning the aluminum content, we can develop the catalyst with the desired catalytic property. Catalyst developed in such a manner was found to be highly active and selective. The products obtained were good and satisfactory. Additionally, the synergistic effect of the bimetals (Cu and Al) in the nanoporous catalysts controls the selectivity of the final products.</span></div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com1tag:blogger.com,1999:blog-6566574378361974711.post-18706449677105599052013-10-03T16:58:00.002-03:002021-03-21T08:44:49.082-03:00Nobel Advice<div dir="ltr" style="text-align: left;" trbidi="on">
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<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgW7ThMRYGILGtab2o_8OshEYxnSo1dGQGWG6IP2kddVoPCww09T9fLSAZwmyV0XHUmA8sXfCWmQvJG6zIJfdrzK59QbBAj0kbbcRnhMCSBYh9rSPWSviemPN03n_-ZySPIqmyZ3YIE-1XP/s1600/Flickr_-_Government_Press_Office_(GPO)_-_Nobel_Laureate_Avram_Hershko.jpg" style="clear: left; float: left; margin-bottom: 1em; margin-right: 1em;"><img border="0" height="320" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgW7ThMRYGILGtab2o_8OshEYxnSo1dGQGWG6IP2kddVoPCww09T9fLSAZwmyV0XHUmA8sXfCWmQvJG6zIJfdrzK59QbBAj0kbbcRnhMCSBYh9rSPWSviemPN03n_-ZySPIqmyZ3YIE-1XP/s320/Flickr_-_Government_Press_Office_(GPO)_-_Nobel_Laureate_Avram_Hershko.jpg" width="244" /></a></div>
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Are you a Nobel aspirant, young researcher, or want to be part of good science? Here is an advice from <a href="http://en.wikipedia.org/wiki/Avram_Hershko">Prof. Avram Hershko</a> ( Winner of 2004 Nobel Prize -for the discovery of ubiquitin-mediated protein degradation)</div>
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Here is a lesson from his life in science that he presented at the Lindau Nobel Meeting 2013."</div>
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<li style="text-align: justify;">It is very important to have good mentors- you cant learn how to do good science just from reading the literature.</li>
<li style="text-align: justify;">Find an important subject that is not yet interesting to others the big guys will get there before you! Do not go with the mainstream. </li>
<li style="text-align: justify;">Accidental observations may be the most important ones. Grab your Luck. </li>
<li style="text-align: justify;">Use whatever experimental approach is needed for your objective. It may not necessarily be the most fashionable (“state-of-the-art”) technology. Of course, biochemistry will always be needed. </li>
<li style="text-align: justify;">Science should be a curious driven adventure. You should have a lot of excitement and fun. </li>
<li style="text-align: justify;">Never leave bench work, and shall continue to get a lot of excitement and fun.</li>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com0tag:blogger.com,1999:blog-6566574378361974711.post-90651694202939671492013-06-30T19:46:00.001-03:002020-07-11T13:28:05.783-03:00Inspired by Nobel<div dir="ltr" style="text-align: left;" trbidi="on">
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It is a great honor, not to mention my good fortune as well, to be nominated and sponsored by <a href="http://www.dst.gov.in/">Department of Science and Technology, India,</a> as one of the 23 young researchers who will be attending the <a href="http://www.lindau-nobel.org/2013_Lindau_Meeting__Chemistry.AxCMS">63rd Lindau Nobel Laureate Meeting</a> as part of the Indian delegation.</div>
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With much anticipation, I await to listen to the eminent speakers at the <a href="http://www.lindau-nobel.org/upload/Programme_63rd_Lindau_Nobel_Laureate_Meeting_MEDRES_8021.pdf">Lindau stellar</a>, who need no elaborate introduction. The work of most of the scholars have formed a basis for my own work as well as for thousands of other scientists and students around the world. We ceaselessly draw inspiration from their work. I have long admired these scholars, but to listen to them in person would be an awe-inspiring experience, which I am sure would vouch for it.</div>
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“It is the quest for knowledge that drives the scientific community.” Armed with this belief, I look forward to meet and interact with personalities of scientific excellence at close quarters. The informal setting at the Lindau Meeting, I hope, will allow us to discuss our work in a relaxed manner. I believe this meeting will be a great platform to learn directly from the <a href="http://www.lindau-repository.org/public/ParticipantDirectory2013.pdf">masters and to meet peers</a> from across the globe.</div>
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Read More at the <a href="http://lindau.nature.com/lindau/2013/06/the-quest-for-knowledge-2/">Lindau blogs website</a></div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com1Lindau, Germany47.5626274374099 9.71328735351562547.4769269374099 9.5519258535156251 47.6483279374099 9.8746488535156249tag:blogger.com,1999:blog-6566574378361974711.post-55801968472631289342013-05-08T09:26:00.002-03:002021-03-21T08:48:30.949-03:00Click Chemistry for Pyrrole Synthesis<div dir="ltr" style="text-align: left;" trbidi="on">
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The <a href="http://en.wikipedia.org/wiki/Pyrrole">Pyrrole</a> heterocycle is an important chemical motif, found widely in pharmaceuticals, natural products, agrochemicals, and advanced materials. The introduction of new methods or further the work on technical improvements in order to overcome the limitations (such as low efficiency and selectivity) found in pyrrole synthesis is still a pressing experimental challenge. </div>
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<span style="text-align: justify;">The concept of “<a href="http://en.wikipedia.org/wiki/Click_chemistry">Click Chemistry</a>” is gaining rapidly due to its high efficiency, selectivity, and yield under mild reaction conditions with a wide variety of readily available starting materials. The copper-catalyzed azide-alkyne cycloaddition (CuAAC) has emerged as the premier example of click chemistry and plays a significant role in organic synthesis. </span><br />
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<a href="http://202.114.73.59/GCI_Website/?page_id=181">Prof. Aiwen Lei </a>and coworkers, Wuhan University, Hubei, have developed a <a href="http://onlinelibrary.wiley.com/doi/10.1002/ange.201302604/abstract">silver catalyst “click reaction” </a>for the synthesis of pyrrole, by cycloaddition. This system benefits from readily-available starting materials, low catalyst loading (0.1 eq), short reaction times (2 h), and excellent chemo-selectivity. Moreover it works for both internal and alkyl-substituted terminal alkynes in the presence of many functional groups. The extremely mild conditions used make this reaction synthetically attractive. </div>
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This mechanism involves the formation of silver–acetylide complex and silver–isocyanide complex. Subsequently, the cyclo-addition between complexes would afford the key intermediate complex to be followed by protonation and tautomerization of the intermediate complex to form the desired product. </div><div style="text-align: justify;"><span style="color: #0e101a; text-align: start;"><br /></span></div><div style="text-align: justify;"><span style="color: #0e101a; text-align: start;">The catalytic synthesis protocol tolerates many functional groups, including methylthio, methylsulfonyl, and ethynyl groups. Moreover, alkyl-substituted terminal alkynes were also found to be suitable reaction partners. Interestingly, both Cu(II) and Cu(I) turned out to be ineffective.</span></div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com0tag:blogger.com,1999:blog-6566574378361974711.post-84272859221838037992013-02-17T07:09:00.004-04:002021-03-23T03:09:18.955-03:00 Useful chemicals and fuel from carbon dioxide<div dir="ltr" trbidi="on">
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</div><div style="text-align: justify;">Carbon dioxide is an abundant, non-toxic, inexpensive, and renewable source of carbon. This makes CO2 the most coveted compound by Green Chemistry enthusiasts. Industries are always on the lookout for ways to enable the effective use of to act as synthetic building blocks for producing fuels like Methane, Di-methyl-ether, and Methanol fine-chemicals. Furthermore, CO2 conversion could also help reduce atmospheric CO2 levels, popularly known as “Green House Gas”, and thus, protect the climate.</div><div class="MsoNormal" style="line-height: 150%; mso-layout-grid-align: none; text-align: justify; text-autospace: none;"><span face="-webkit-standard, serif" style="color: #0e101a; text-align: start;"><br /></span></div><div style="text-align: justify;">Nature has been highly successful in using CO2 as synthetic building blocks in photosynthesis. For decades, scientists have been trying to understand this phenomenon at a molecular level. Such studies have proved useful in developing biomimetic catalysts for CO2 conversion. Chlorophyll (Porphyrin molecules) in green plants convert incident sunlight and atmospheric CO2 into sugars (energy). So, this makes them a promising target for testing activation catalysts for CO2 adsorption. Effective CO2 adsorption using man-made catalysts is indeed our end-goal. Much research is being conducted in this area to further the economic viability of the processes that utilize CO2. Several companies are pursuing the idea/concept of thermochemical and electrochemical conversion of CO2 into chemical feedstock or polymers. Research and development are currently focused on increasing the catalyst life and bringing down the temperature of conversion.</div> <div style="text-align: justify;"><br /></div><div style="text-align: justify;">Future research must emphasize the rational design of highly active catalysts to satisfy the economic development of CO2 conversion. However, the development of such efficient catalysts requires a complete understanding of CO2 and CO2-catalyst interactions.</div><div class="MsoNormal" style="line-height: 150%; mso-layout-grid-align: none; text-align: justify; text-autospace: none;"><br /></div><div class="MsoNormal" style="line-height: 150%;">In order to develop such a catalyst, the following points should be considered,</div><div class="MsoNormal" style="line-height: 150%;"><ol style="text-align: left;"><li>CO2 has a strong affinity towards nucleophiles and electron-donating reagents due to its carbonyl-carbon's electron deficiency; if the designed <a href="https://www.blogger.com/#">catalysts</a> has nitrogen or base-functionality (basic), it will have an increased affinity towards CO2 (e.g., Porphyrin, Grignard reagents).</li><li>With low-valent metals and alkene, CO2 undergoes “oxidative cycloaddition.”</li><li>New CO2 soluble catalysts may increase efficiency.</li><li>Homogeneous catalysis in compressed CO2 may increase selectivity.</li><li>The catalyst in supercritical CO2 may also increase stability. It is essential to use CO2, based on the unique physical properties as that of the supercritical fluid, either as a solvent, or as an anti-solvent, or reactant, or a combination of all.</li><li>Photoelectrochemistry, the study of using solar energy to split CO2, is an emerging method for <a href="https://www.blogger.com/#">clean production of chemicals</a>. It is also essential to develop catalysts (Semiconducting materials) for the electrochemical conversion of CO2.</li><li>The use of high-energy starting materials may ease the catalyst role.</li><li>The catalyst will be more efficient if it has both CO2 adsorption and activation functionality. E.g., designer MOF that contains <a href="https://www.blogger.com/#">Lewis-base sitewill donate electron to CO2</a>, in contrast to the Lewis-acids sites in traditional MOFs for adsorbing CO2.</li><li>A computational tool such as Density Function Theory (DFT) may help improve the catalytic activity or find a new catalyst.</li><li>Chemical reactions can also benefit from using CO2 as a mild oxidant or as a selective source of O2 atoms because dissociation of CO2 on a catalyst-surface could produce active O2 species.</li></ol><span style="color: #0e101a;"><div style="text-align: justify;">The trend towards converting CO2 to valuable chemicals and fuels will probably intensify in the near future. This could, in turn, lead to effective management to tackle climate change and the energy crisis.</div></span><p style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt;"><br /></p>As Whitesides <a href="https://www.blogger.com/#">emphasizes</a>, managing CO2 and conversion into valuable chemicals and energy will be the reinvention of chemistry, and it is also a chemistry/ molecular solution to the critical problem facing society. He says<p style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt;"><br /></p><p style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt;"><em style="margin-bottom: 0pt; margin-top: 0pt;"> “Some of the most interesting problems in science, and many of the most important facing society, need chemistry for their solution. Examples include: understanding life as a network of chemical reactions; interpreting the molecular basis of disease; global stewardship; the production, storage, and conservation of energy and water; and the </em><strong style="margin-bottom: 0pt; margin-top: 0pt;"><em style="margin-bottom: 0pt; margin-top: 0pt;">management of carbon dioxide.</em></strong><em style="margin-bottom: 0pt; margin-top: 0pt;">"</em></p><br /><div style="text-align: justify;">Issues pertaining to CO2 are <a href="https://www.blogger.com/#">truly global</a> and a major opportunity to develop sustainable energy options and environmental preservation. So, the use of CO2 to synthesize useful chemicals & fuels will mark a new field in chemistry. It is important to establish university-industry-collaboration to search for new-reactions & new-catalysts in this field.</div></div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com11tag:blogger.com,1999:blog-6566574378361974711.post-45973417463511112992013-02-02T09:10:00.001-04:002020-07-11T13:31:04.721-03:00Hope for Drug to Reduce Old-Age-Related Muscle Wasting<div dir="ltr" style="text-align: left;" trbidi="on">
<b>Guest Post – Lily Bryant</b><br />
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The results of a study carried out by researchers at the Center of Regenerative Medicine at Massachusetts General Hospital in Boston, USA, and the Department of Craniofacial Development and Stem Cell Biology at King’s College London, England, indicate that a cure for <a href="http://muscle%20weakening/">muscle weakening</a> caused by old age might be on the horizon. Muscle wasting is an inevitable symptom of growing older. It can be slowed down by <a href="http://articles.timesofindia.indiatimes.com/2012-09-06/fitness/31625793_1_slow-muscle-heart-failure-muscle-breakdown">regularly exercising</a> but there is no known way of reversing it at the moment. This looks set to change though, as the researchers have treated old mice with a drug that has significantly improved the ability of their aged muscle tissue to self-repair. </div>
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<b>Fibroblast Growth Factor 2 </b></div>
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Strenuous activity, such as doing press-ups or lifting weights, results in a small level of damage to the muscles. Stem cells are triggered to repair them by dividing and developing into new muscle fibers. This results in <a href="http://fatgripz.com/">big arms</a> and rippling torsos. However, weakening of the muscles due to old age means that <a href="http://www.gerontologyindia.com/pdf/vol-21-3.pdf">bulging biceps</a> can soon become puny and weak. This occurs because as people grow older, their muscle loses its ability to regenerate. A study conducted by the University of Potsdam in Germany indicates that people lose just under a third of their muscle strength between the ages of fifty and seventy. The researchers at Massachusetts General Hospital and King’s College London deduced that this is due to the fact that the number of dormant stem cells in muscles decreases with age. They concluded that in mice, this was caused by excessively high levels of a protein that stimulates cells to divide, known as<a href="http://en.wikipedia.org/wiki/Fibroblast_growth_factor_2"> fibroblast growth factor 2</a> (FGF2). </div>
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<b>Preventing Muscle Stem Cell Decline </b></div>
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In aging muscle, fibroblast growth factor 2 was found to be continuously awakening dormant stem cells for no reason. The stem cell supply was observed to deplete over time, meaning that an insufficient number were available when they were really needed. As a result of this, muscle regeneration ability was impaired. The researchers discovered that using a drug called SU5402 that inhibits fibroblast growth factor 2 can prevent muscle stem cell decline in aging mice. Treating the elderly rodents with this drug increased their ability to repair muscle tissue. </div>
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<b>Reducing the Impact of Old Age </b></div>
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<a href="http://rg.kcl.ac.uk/staffprofiles/staffprofile.php?pid=20">Dr Albert Basson,</a> who is a senior researcher at King’s College London, has stated that the findings mean that treatments that could make old muscles young again could one day be developed, thus reducing the impact of old age. He says that if such a treatment came into existence, people would be able to live more independent, mobile lives as they grew older. Senior author Dr Andrew Brack of Massachusetts General Hospital says that just as it is important for athletes to schedule recovery into the time that is taken for training, stem cells require time in which to recuperate but elderly cells recuperate less often. Scientists are yet to figure out why it is that levels of fibroblast growth factor 2 increase causing excessive stem cell activation as people get older. Research team member Kieran Jones of King’s College London says that the next step is to conduct an analysis of old muscle in humans in order to see whether or not the same mechanism is responsible for the depletion of stem cells in human muscle fibers leading to wasting and loss of mass. </div>
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<b>The Implications of the Research </b></div>
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Once it has been confirmed that stem cells in human muscle fibers are negatively affected by fibroblast growth factor 2, work can start on introducing a drug to the market that will stop the process from taking place and consequently reduce the extent to which elderly people are immobilized and prevented from doing what they want to do by the effects of age-related muscle weakening. The average life expectancy in India has increased by over four and a half years since 1998. Now that people are living longer than they used to live for, a drug that reduces the amount to which becoming elderly negatively impacts upon the quality people’s lives would be extremely beneficial. It would mean that individuals who have reached the later stages of their lives could enjoy the time that they have left without having their independence limited by their muscles becoming increasingly weak and feeble.</div>
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<b>About Lily Bryant</b></div>
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Lily Bryant is a writer working with one of only two licensed online pharmacies in the US. She is strongly interested in promoting and creating content aimed at relevant readers as part of her role in ethical healthcare business. She believes that it is important that we play a strong role in leading society towards a healthier lifestyle through the promotion of exercise and healthy diet rather than an early adoption of drug treatment.</div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com7tag:blogger.com,1999:blog-6566574378361974711.post-15142190226517090342013-02-01T12:07:00.002-04:002021-03-21T08:52:34.960-03:00Artificial Photosynthesis using graphite Carbon Nitride<div dir="ltr" style="text-align: left;" trbidi="on">
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Fine chemicals and hydrogen production from water, carbon dioxide, and solar energy are ideal future chemical and energy sources independent of fossil reserves. The development of new functional molecular materials (catalyst) for the application in fine chemical and clean energy production using water and solar energy is fascinating and quite challenging because the catalyst must be sufficiently efficient, stable, inexpensive, and capable of harvesting light. </div>
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Polymeric <a href="http://en.wikipedia.org/wiki/Graphitic_carbon_nitride">graphite carbon nitride</a> (<span style="font-family: "times new roman", serif; font-size: 12pt; line-height: 115%; mso-ansi-language: EN-US; mso-bidi-language: AR-SA; mso-fareast-font-family: Calibri; mso-fareast-language: EN-US; mso-fareast-theme-font: minor-latin;">C<sub>3</sub>N<sub>4</sub></span>) materials are commonly available simple semiconductor photocatalysts. It is being non-volatile up to <span style="font-family: "times new roman", serif; font-size: 12pt; line-height: 115%; mso-ansi-language: EN-US; mso-bidi-language: AR-SA; mso-fareast-font-family: Calibri; mso-fareast-language: EN-US; mso-fareast-theme-font: minor-latin;">600<sup>0</sup>C</span> even in the air with no detectable solubility or reactivity in conventional solvents, including water, alcohols, DMF, THF, diethyl ether, and toluene. Carbon nitride is considered to be extremely stable and basic in nature. It can be used as the multifunctional heterogeneous catalyst for fine chemical and pharmaceutical synthesis as well as a good organic semiconductor due to its right bandgap (2.7 eV corresponding to an optical wavelength of 460 nm). </div>
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Prof. Markus Antonietti and his team at <a href="http://www.google.co.in/url?sa=t&rct=j&q=prof.%20markus%20antonietti&source=web&cd=1&cad=rja&ved=0CC4QFjAA&url=http%3A%2F%2Fwww.mpikg.mpg.de%2Fenglish%2F03-colloidChemistry%2Fdirector%2FCurriculum_Vitae%2Findex.html&ei=K5UKUZyrAsjJrAf8poHYCQ&usg=AFQjCNHZhF2ZxJGwp7XShaEbCuMvNqLdwQ">Max Planck Institute of Colloids and Interfaces</a> in Germany, have successfully <a href="http://onlinelibrary.wiley.com/doi/10.1002/anie.200603478/abstract">split CO2</a> or <a href="http://www.nature.com/nmat/journal/v8/n1/abs/nmat2317.html">photochemically</a> turn water into hydrogen and oxygen using graphite carbon nitride. However, only four micromoles of hydrogen per hour were produced out of the researcher's reaction vessel (quantum efficiency of the Pt modified CN is approximately 0.1% with irradiation of 420-460 nm). This opens the door to artificial photosynthesis and produces chemicals and energy from greenhouse gas /solar energy. It will contribute to the prevention of global climate change. </div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com1tag:blogger.com,1999:blog-6566574378361974711.post-35130988448973698152013-01-23T04:21:00.002-04:002021-03-23T03:10:17.611-03:00Harmless Viruses Might be a Potential Treatment for Acne<div dir="ltr" style="text-align: left;" trbidi="on">
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<b>Guest Post – Lily Bryant</b></div>
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According to a report published in the <a href="http://www.ijdvl.com/article.asp?issn=0378-6323;year=2009;volume=75;issue=7;spage=1;epage=2;aulast=Kubba">Indian Journal of Dermatology, Venereology and Leprology</a>, there are thought to be between two million and three million acne sufferers in India. Acne can lead to low self-esteem and image problems and is the scourge of teenage boys all over the country. Fortunately towards the end of 2012, researchers at the University of California, Los Angeles, and the University of Pittsburgh in the United States discovered that phages living on our <a href="http://www.healthzillion.com/acne/propionibacterium-acnes/">skin possess </a>the ability to kill <a href="http://en.wikipedia.org/wiki/Propionibacterium_acnes">propionibacterium acnes,</a> which is the virus that causes it. This could be good news for those whose skin is tarnished by this condition and mean that an end is in sight.</div>
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<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhIEdJ9GsiMbraQq__iFqLgWGV3cG08cSpQpKJWnC3cD1QaukF6LIVuiKfOPbh1-DyrB3Fu3hWhP_-Eh5YVscmFx8bYuNpqPFLkQ9b_KEDdllDZsPZBBprciImdnYtz6EEyr8CtmTLFjITI/s1600/propionibacterium-acnes.jpg" style="clear: left; float: left; margin-bottom: 1em; margin-right: 1em;"><img border="0" height="152" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhIEdJ9GsiMbraQq__iFqLgWGV3cG08cSpQpKJWnC3cD1QaukF6LIVuiKfOPbh1-DyrB3Fu3hWhP_-Eh5YVscmFx8bYuNpqPFLkQ9b_KEDdllDZsPZBBprciImdnYtz6EEyr8CtmTLFjITI/s200/propionibacterium-acnes.jpg" width="200" /></a></div>
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There has been a rapid increase in the promotion of drugs aimed at enhancing individuals’ physical appearances in recent years. The <a href="http://www.franchiseindia.com/magazine/2012/july/WEALTH-IN-WELLNESS_89-1-1/">weight loss</a> industry has grown at a yearly rate of over twenty-five percent, with more people than ever purchasing diet pills and <a href="http://www.ironscience.co.uk/prorange/islean.html">fat burners</a>, the hair loss treatment industry has been growing by one percent per year and the acne treatment industry has also seen significant growth. People’s daily lives are affected in a major way by how they look so a cure for acne could be both highly profitable for the pharmaceutical company that is responsible for it and highly beneficial to sufferers.</div>
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In order to arrive at their discovery, the researchers at the two universities analysed phages and deduced that they make endolysin, which breaks down propionibacterium acnes before killing it. They also discovered that the phages shared eighty-five percent of their DNA. This is unusual for viruses and means that when used as a treatment, it would be unlikely that immune resistance would develop.</div>
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<b>Advantages Over Other Forms of Treatment</b><br />
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<span style="text-align: justify;">Unlike antibiotics, which kill many different types of bacteria including ones that live in the gut and can have positive effects, phages are programmed to only target specific bacteria. According to director of the University of California, Los Angeles, Clinic for Acne, Rosacea and Aesthetics Dr Jenny Kim, who was one of the researchers, many acne strains are now resistant to antibiotics such as tetracycline, as they are so widely used. Drugs like </span><i style="text-align: justify;">Accutane </i><span style="text-align: justify;">are still effective but can have risky side effects, which limits their use. The researchers at the two universities have stated that phages could offer a tailored therapy that has less adverse side effects. Therefore phages could be the new form of acne medication that those inflicted with the condition have been looking for.</span></div>
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<b style="text-align: justify;">Development of New Drugs and Treatments </b></div>
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Study co-author Graham Hatfull, who is a biotechnology professor at the University of Pittsburgh, has stated that there are two ways in which this research could be used with regards to the development of new drugs and treatments. He says that phages could either be used directly as therapy for acne or phage-based components could be utilized. Professor Hatfull also says that the work that the University of California, Los Angeles, and the University of Pittsburgh have carried out has provided the world with useful information about phages and paved the way for the thinking up of potential applications for them. He points out that whilst acne is a condition that a significant percentage of the population is likely to suffer from at some point in their lives, there are still currently few effective methods for curing it. Hatfull says that harnessing a virus that naturally preys upon the bacteria that causes spots looks to be a promising means of reducing both the physical and the mental scars that acne can inflict upon individuals.</div>
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<b>Implications of the Research</b></div>
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It appears that being forced to endure pimples and spots could soon bee a thing of the past. The results of a study published in the Journal of Cosmetic Dermatology in 2010 demonstrate that acne can severely negatively impact upon the self-esteem of sufferers and increase the risk of them developing psychological disorders. It can make them two to three times more likely to become clinically depressed. Therefore it is high time that there was a means of treating it and phages could provide the answer. Now it is just a matter of deciding what the best way of using them to gain the optimum results in acne reduction is<span style="color: #500050; line-height: 150%;">.</span></div>
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<b> About Lily Bryant</b></div>
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<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgOFkUorbOPJXdSEx0EOh4TG-2A4aZKzEQNgG3O8Q5pU6ySVGYTwxRncx_bf4sBASuLEO_T0aKudyxSW8h0kH4CyYmU_DY6tf5kxpBKQbPgJ7nWITK4Y2dX-XnCqvlCAl6OeYYF01WjYuXf/s1600/Lily-McCann1.jpg" style="clear: left; float: left; margin-bottom: 1em; margin-right: 1em;"><img border="0" height="200" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgOFkUorbOPJXdSEx0EOh4TG-2A4aZKzEQNgG3O8Q5pU6ySVGYTwxRncx_bf4sBASuLEO_T0aKudyxSW8h0kH4CyYmU_DY6tf5kxpBKQbPgJ7nWITK4Y2dX-XnCqvlCAl6OeYYF01WjYuXf/s200/Lily-McCann1.jpg" width="181" /></a></div>
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Lily Bryant is a writer working with one of only two licensed online pharmacies in the US. She is strongly interested in promoting and creating content aimed at relevant readers as part of her role in ethical healthcare business. She believes that it is important that we play a strong role in leading society towards a healthier lifestyle through the promotion of exercise and healthy diet rather than an early adoption of drug treatment.</div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com5tag:blogger.com,1999:blog-6566574378361974711.post-71122982084728742432013-01-20T22:51:00.003-04:002021-03-21T07:16:31.961-03:00Modulators of Protein–Protein Interactions<div dir="ltr" style="text-align: left;" trbidi="on">
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<a href="http://onlinelibrary.wiley.com/doi/10.1002/anie.201107616/abstract">Protein-protein interactions (PPI)</a><span data-preserver-spaces="true" style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: left;"> play a crucial role in most biological processes. This nature of PPI has put forward itself as a prospective candidate for therapeutic intervention. Traditional small molecule target classes such as Enzymes, GPCRs, Kinases, etc. have a deep pocket (often used to bind an endogenous substrate), where small molecules tend to bind. On the other hand, PPIs appear to be too large and featureless for small molecules to bind against. Hence, due to this lack of well-defined binding pockets, they were considered unsuitable/ extremely hard for targeting small molecules. </span></div><p style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt;"><br /></p><p style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt;"><span data-preserver-spaces="true" style="margin-bottom: 0pt; margin-top: 0pt;">Attempts at generating small molecule modulators of PPIs have been largely unsuccessful by adopting existing chemical techniques. This leads us to believe that we need to identify novel chemical space that can leverage the flat and expansive surfaces of PPI, which would in turn provide an effective binding for small molecules. However, pharmaceutical companies are rather unwilling to add compounds containing multiple rings, multiple stereocenters that are highly complex, into their corporate collection as it does not align with their immediate short-term business goals.</span></p>
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<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEg91KhaGqGsHGUEQHlQP0-rmk29HqeUTCOrVWjsvNmha6f3Rh2QajEveMEFvvdHcO-DJoPx90n70LgW8wJAKvdnmAvyQiPyrtqZ0-ZblWz0kCfUJ7dKSd74TX4zgBFR_c5KPT3E49HRSeGh/s1600/dd.gif" style="clear: left; float: left; margin-bottom: 1em; margin-right: 1em;"><img border="0" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEg91KhaGqGsHGUEQHlQP0-rmk29HqeUTCOrVWjsvNmha6f3Rh2QajEveMEFvvdHcO-DJoPx90n70LgW8wJAKvdnmAvyQiPyrtqZ0-ZblWz0kCfUJ7dKSd74TX4zgBFR_c5KPT3E49HRSeGh/s1600/dd.gif" /></a></div><div>Dr. Prabhat Arya is <a href="https://pubs.acs.org/doi/10.1021/ol3032126">developing</a> a new chemical toolbox enriched with both Heterocyclic Compounds and Natural Products to tackle such issues from Dr. Reddy’s Institute of Life Sciences. This approach could create a large 3D surface area, numerous binding interactions, rich stereochemical diversity, which would, in turn, solve the poor cell permeability of natural products, not to mention the added advantage of overcrowded IP Space.</div><div><br /></div><div>The field of small-molecule-PP interactions appears to be highly promising, and in the near future, we can hope to see several strategies and techniques that will pave the way towards discovering novel agents in this regard.</div></div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com1tag:blogger.com,1999:blog-6566574378361974711.post-8052026377278386322012-11-07T11:34:00.005-04:002021-03-21T07:11:45.929-03:00Key Concepts for Medicinal ChemistsMolecular recognition in biological systems occurs by the complementary non-covalent bonding between a receptor binding site and a ligand (e.g., drug molecule). The attached concepts, numbers, and formulae assist medicinal chemists in structural modification related to the drug-receptor binding. <div dir="ltr" trbidi="on"><br />
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com1tag:blogger.com,1999:blog-6566574378361974711.post-72851059117747239292012-05-28T10:47:00.001-03:002021-03-21T07:09:39.146-03:00Picture of Olympicene<div dir="ltr" style="text-align: left;" trbidi="on">
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Back in <a href="http://news.bbc.co.uk/2/hi/science/nature/8225491.stm">2009</a>, at the IBM Research lab scientists imaged, for the first time, the chemical structure of an individual molecule (pentacene) with unprecedented resolution, using technique they developed called <a href="http://en.wikipedia.org/wiki/Atomic_force_microscopy">noncontact atomic force microscopy</a>. The same IBM team, has once again come up with an interesting image. This time they have imaged a new organic molecule, Olympicene.<br />
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Olympicene, gets its name because its five linked rings resemble the Olympic symbol. The compound is a powder, that is very sensitive to light. In fact, even with brief exposure it changes color. It is only 1.2 nanometers wide, or 100,000 times thinner than a human hair. This AFM technique could become a real structure-determination tool for organic chemist.<span style="background-color: white;">
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com0tag:blogger.com,1999:blog-6566574378361974711.post-7819121726128090122012-05-17T01:37:00.003-03:002021-03-21T07:08:33.076-03:00PhD student fellowships<div dir="ltr" style="text-align: left;" trbidi="on">
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</div>Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com0tag:blogger.com,1999:blog-6566574378361974711.post-57707545074905262032012-05-16T11:18:00.003-03:002021-03-21T07:02:45.534-03:00Molecule vending machine<div dir="ltr" style="text-align: left;" trbidi="on">
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Nano-catalysis is a fast-growing field of chemistry, which involves the use of nanomaterials as catalysts for a variety of selective organic transformations. Nano-catalysis can be considered as a bridge between homogeneous and heterogeneous catalysis. Because of the high surface area of nanomaterials, the contact between reactants and catalyst increases dramatically, and they can operate in the same manner as homogeneous catalysts (homogeneous catalysis); at the same time, due to their insolubility in the reaction solvent, they can be separated out easily from the reaction mixture (heterogeneous). Only the molecules of certain sizes and chemical properties are selected and guided to the reaction centers, where they are efficiently transformed into the desired products.</div><div class="MsoNormal" style="text-align: justify;"><br /></div><div class="MsoNormal" style="text-align: justify;">Solid supports have the potential to house more than one metal and, hence, catalyze multiple types of bond constructions. Such “multifunctional” catalysts attained much attention due to several advantages over mono metal catalysts. The high selectivity of the nanocatalyst may help reduce the energy consumption required for product separation and waste disposal processes in chemical industries.</div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com0tag:blogger.com,1999:blog-6566574378361974711.post-75316714974569729082012-01-22T22:40:00.002-04:002021-03-21T07:01:07.800-03:00Totally drug-resistant TB<div dir="ltr" style="text-align: left;" trbidi="on">
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<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhb3meFwod0KsuiohW3e-Bmcn2m-oU6Kous8kYcepLVkKMEAb7CdNT3Um9Js3X5-PzX2r2G0qAtJqu_B7g45WXmnxHIN4cD12MxWL0GxEx6GHmApozTv47QpzH_b756BsyHjn0qO40vAY4J/s1600/tb1.gif" style="clear: left; float: left; margin-bottom: 1em; margin-right: 1em;"><img border="0" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhb3meFwod0KsuiohW3e-Bmcn2m-oU6Kous8kYcepLVkKMEAb7CdNT3Um9Js3X5-PzX2r2G0qAtJqu_B7g45WXmnxHIN4cD12MxWL0GxEx6GHmApozTv47QpzH_b756BsyHjn0qO40vAY4J/s1600/tb1.gif" /></a></div><div class="MsoNormal">One of the biggest problems in Tuberculosis (TB) therapy nowadays is that patients have to take antibiotics for up to 9 months. As many patients feel better before this time, they prematurely stop their treatment, leaving pools of the most drug-resistant M. tuberculosis in their lungs. This contributes to the emergence of complete drug resistance in future patients.</div><div class="MsoNormal">In the past few years, strains of drug-resistant Mtb have become prevalent. In fact, resistance is so widespread that it is now being classified as multi-drug resistant (MDR-TB) and extreme-drug resistant (XDR-TB). Two of the world’s most populous countries, India and China, account for more than 50% of the world’s MDR-TB cases.</div><div class="MsoNormal"><br /></div><div class="MsoNormal">Recent reports have also confirmed a new Mtb strain that is completely untreatable and has been designated as Totally drug resistance TB (TDR-TB). Indeed, strains of Mtb have even evolved resistance to all major available anti-TB drugs. India (2012) is the third country in which a total drug-resistant form of TB has emerged, following cases documented in Italy in 2007 and Iran in 2009. There is a need for a more readily available treatment that is effective against both sensitive and drug-resistant strains of M. tuberculosis is evident.</div></div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com15tag:blogger.com,1999:blog-6566574378361974711.post-82559659090456510762012-01-22T06:16:00.001-04:002021-03-21T06:59:14.271-03:00Nano reactions<div dir="ltr" style="text-align: left;" trbidi="on"><br />
<div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgj8Dd8VQTmZVGeCOyzNuIq9KmzZOQJcUHkTboLc3QjSx7W2VIvvKLmh_n4IazODfgXIaxcRlyRgp48LpsjAbYSpceqWD5HNH-DJ3By2IL63mUyT8mJhVI2R1GXRjnnUJCp_55X9wcR4OG9/s1600/nano+rection.bmp" style="clear: left; float: left; margin-bottom: 1em; margin-right: 1em;"><img border="0" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgj8Dd8VQTmZVGeCOyzNuIq9KmzZOQJcUHkTboLc3QjSx7W2VIvvKLmh_n4IazODfgXIaxcRlyRgp48LpsjAbYSpceqWD5HNH-DJ3By2IL63mUyT8mJhVI2R1GXRjnnUJCp_55X9wcR4OG9/s1600/nano+rection.bmp" /></a></div><div style="text-align: justify;">Recently, <a href="http://en.wikipedia.org/wiki/Nanoporous">nanoporous</a> <span style="color: #0e101a; text-align: start;">materials have emerged as important and efficient heterogeneous catalysts for organic transformations due to their excellent textural characteristics, including high surface area, large pore volume, uniform pore size distribution, and simplicity in workup recyclability. The pore diameters are chosen to control the access of molecules to the catalytic reaction sites located inside the porous cavities. Only the molecules of specific sizes and chemical properties are selected and guided to the reaction centers, where they are efficiently transformed to the desired products.</span></div></div>Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com0tag:blogger.com,1999:blog-6566574378361974711.post-12934462984978904972012-01-20T09:28:00.001-04:002021-03-21T06:56:58.850-03:00What is a PhD worth?<div dir="ltr" style="text-align: left;" trbidi="on"><div style="text-align: left;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEiB2lNPhRZXGrHc8Ka06v50Rgd_3odDa7oI_uhvdRIwzQlb1anSDWh0nBKCmru1xgKCvmmesMzGasLHh3_ilRGKf_aKfHN24z40cjWaMdO2J8-pZ1zkedXfQw_XP8Z3yCdZwlFX2UhVcfJV/s1600/PhD960.jpg" style="clear: left; float: left; margin-bottom: 1em; margin-right: 1em;"><img border="0" height="320" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEiB2lNPhRZXGrHc8Ka06v50Rgd_3odDa7oI_uhvdRIwzQlb1anSDWh0nBKCmru1xgKCvmmesMzGasLHh3_ilRGKf_aKfHN24z40cjWaMdO2J8-pZ1zkedXfQw_XP8Z3yCdZwlFX2UhVcfJV/s320/PhD960.jpg" width="276" /></a></div><p style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt;"><span data-preserver-spaces="true" style="margin-bottom: 0pt; margin-top: 0pt;">Here is another </span><span data-preserver-spaces="true" style="margin-bottom: 0pt; margin-top: 0pt;"><a href="http://www.nature.com/news/2011/110420/full/472276a.html">article</a><span style="caret-color: rgb(0, 0, 0); color: black;"> </span> in nature that makes some good points about the worth of a Ph.D.</span></p><p style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt;"><br /></p><p style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt;"><span data-preserver-spaces="true" style="margin-bottom: 0pt; margin-top: 0pt;">"</span><em style="margin-bottom: 0pt; margin-top: 0pt;">The number of science doctorates earned each year grew by nearly 40% between 1998 and 2008, to some 34,000, in countries that are members of the Organisation for Economic Co-operation and Development (OECD). The growth shows no sign of slowing: most countries are building up their higher-education systems because they see educated workers as a key to economic growth. But in much of the world, science Ph.D. graduates may never get a chance to take full advantage of their qualifications</em><span data-preserver-spaces="true" style="margin-bottom: 0pt; margin-top: 0pt;">"</span></p><p style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt;"><br /></p><p style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt;"><span data-preserver-spaces="true" style="margin-bottom: 0pt; margin-top: 0pt;">Ph.D. program used to be for science-loving driven people, and the world wants more innovation from academic science to solve global problems.</span></p></div>Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com3tag:blogger.com,1999:blog-6566574378361974711.post-54227677226060822412012-01-10T06:52:00.001-04:002021-03-21T06:53:09.304-03:00Mycobacteria and the great wall<div dir="ltr" style="text-align: left;" trbidi="on"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhh1ANAIToCYDczPb7JLFNF-d_VJvNKfEwzmBZaZhhM1W2D31BKvE9yh3OMoWBcENHOJp9VDcnzWsaxtI4865el5bvRElNR8GIVkCtdyl4PnOG92u12DJeznuH07o1sSpPo_VW8kbYCqBt1/s1600/blog.png" style="clear: left; float: left; margin-bottom: 1em; margin-right: 1em;"><img border="0" height="320" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhh1ANAIToCYDczPb7JLFNF-d_VJvNKfEwzmBZaZhhM1W2D31BKvE9yh3OMoWBcENHOJp9VDcnzWsaxtI4865el5bvRElNR8GIVkCtdyl4PnOG92u12DJeznuH07o1sSpPo_VW8kbYCqBt1/s320/blog.png" width="314" /></a><div dir="ltr" style="text-align: justify;" trbidi="on">The mycobacterial cell wall is unique, thick waxy, and hydrophobic, ensuring its survival inside human macrophages by resisting oxidative damages. The waxy, highly impermeable nature of the wall provides the required defense mechanism against antibiotic agents and the host organisms. A key component of the cell wall is mycolic acids. Mycolic acid accounts for up to 60% of the organisms' dry weight, which means that most percentage of mycobacteria is a cell wall. A thorough understanding of the influence of polarity on drug penetration into a highly impermeable mycobacterial cell wall will improve permeability.</div><div dir="ltr" trbidi="on"><br /></div><div dir="ltr" style="text-align: justify;" trbidi="on">The permeation ability of a lipophilic molecule is inversely related to the cell wall's fluidity, which decreases as the length of fatty acids in the mycolic acids layer increases. The permeability barrier presented by this cell envelope is also thought to be why many common antibiotics are ineffective against mycobacteria. Lipophilic drugs, such as fluoroquinolones or rifamycins, pass more quickly through the lipid-rich cell wall and thus are more active.</div><div dir="ltr" trbidi="on"><br /></div><div dir="ltr" trbidi="on">Depending on the library screens towards compounds with a particular physicochemical parameter could be detrimental and decrease the diversity in finding new anti-TB drugs.</div><u1:p></u1:p> <br />
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<a href="http://en.wikipedia.org/wiki/Tuberculosis">Tuberculosis</a> and <a href="http://en.wikipedia.org/wiki/Malaria">Malaria</a> <span style="text-align: left;">are two major global threats; both account for 5 million deaths annually (mostly in developing countries). Despite the worldwide ravages of Tuberculosis and Malaria, chemotherapeutic regimens against these two diseases have remained largely unchanged. There is an urgent need to develop novel, effective, and affordable drugs to treat both diseases because the resistance has developed or is developing to existing therapy. Scientists around the world are seeking new ways to combat the two opportunistic pathogens.</span></div>
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<div style="text-align: justify;"><span style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;">Mycobacterium tuberculosis </span><span data-preserver-spaces="true" style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;">and </span><span style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;">Plasmodium Falciparum are </span><span data-preserver-spaces="true" style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;">causative agents of tuberculosis and </span><span style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;">malaria, respectively. </span><span style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;">B</span><span data-preserver-spaces="true" style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;">oth organisms share enzymatic components</span><em style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;"> </em><span data-preserver-spaces="true" style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;">of the type II fatty acid biosynthetic pathway (FAS-II). Enoyl acyl carrier protein reductase (ENR) is one of the key type II enzymes, has been repeatedly</span><em style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;"> </em><span data-preserver-spaces="true" style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;">validated as an effective antimicrobial target (e.g., INH, diazoborines, triclosan, and thiolactomycin).</span><br />
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com1tag:blogger.com,1999:blog-6566574378361974711.post-88023210711242919202011-03-28T22:50:00.002-03:002021-03-21T06:37:01.154-03:00The Future of Drug Discovery<div dir="ltr" style="text-align: left;" trbidi="on">
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<span style="font-family: Arial; font-size: 10pt;"> </span><span style="text-align: left;">The new technologies promise to fill drug development pipelines with small-molecule candidates unfulfilled, so the pharmaceutical industry is currently undergoing rapid changes. They are moving aggressively into large molecule (biologics) drug development.</span></div><div style="text-align: justify;"><span style="font-family: Arial;"><br /></span></div>
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<span style="font-family: Arial;">"<a href="http://www.epsa-online.org/img/fcke/file/EIPG%20-%20Issue%206%20June.pdf">Drug space</a>” </span><span style="text-align: left;">that is not part of the current drug development includes non-Lipinski NCEs, nanomedicines, nucleic acid-based drugs, etc. will include in the future. One of the major challenges for a medicinal chemist is to find small molecule inhibitors for protein-protein interactions.</span></div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com2tag:blogger.com,1999:blog-6566574378361974711.post-6807257480869982862011-03-06T05:40:00.004-04:002021-03-21T06:33:47.015-03:00Toxicophores Simplified<div dir="ltr" style="text-align: left;" trbidi="on"><div class="separator" style="clear: both; text-align: justify;">Toxicophore is a portion of a chemical structure (molecular functionalities) responsible for the toxic properties of a pharmacologically activity compound. Medicinal chemists study toxicophores to predict and replace the potential reactive moieties in the early drug development process to avoid the drug candidate's later-stage failure. A simplified version of the toxicophores is attached here.</div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgB3zPLHgeeCOdxeXgU9pbaqY11C1v4uzc0F8wt-tw6HDBJaHgzaJhxlub4PesN01S5vZnnX6HrWrfVEt0MZS43AYszL4xL8-QDLBdhO9GI8-RR7qwpnqaJiW7EAkDQm-6fk94fXloOUak4/s1600/riskmh0%255B1%255D.JPG" style="margin-left: 1em; margin-right: 1em;"><img border="0" height="308" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgB3zPLHgeeCOdxeXgU9pbaqY11C1v4uzc0F8wt-tw6HDBJaHgzaJhxlub4PesN01S5vZnnX6HrWrfVEt0MZS43AYszL4xL8-QDLBdhO9GI8-RR7qwpnqaJiW7EAkDQm-6fk94fXloOUak4/w400-h308/riskmh0%255B1%255D.JPG" width="400" /></a></div><br />
</div>Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com2tag:blogger.com,1999:blog-6566574378361974711.post-5663997402205738162010-07-22T10:08:00.003-03:002021-03-21T02:50:07.792-03:00Bottom of the pyramid<div dir="ltr" style="text-align: left;" trbidi="on">
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<div style="text-align: justify;"><span data-preserver-spaces="true" style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;">Indian patients no longer have to wait for the drug to become generic. Recently BMS and Astra Zeneca launched their new oral pill </span><span data-preserver-spaces="true" style="color: #0e101a; margin-bottom: 0pt; margin-top: 0pt; text-align: start;"><a href="http://en.wikipedia.org/wiki/Saxagliptin" style="text-align: justify;">Saxagliptin</a> (DDP 4 inhibitors ) to treat type 2 diabetes in India, less than one year after its US approval. India is the first Asian country where the drug is available at an affordable price which is 1/5 of its US cost.</span></div>
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Pharma Companies now realize that there is tremendous opportunity in emerging markets, not only because they entail low operating costs but also because of the fast-growing middle-class population; they are emerging as a huge market for global products. As the economy grows lifestyle associated diseases grow along with it. Therefore companies try to launch drugs for these lifestyle-related diseases such as diabetes. Forecasts suggest 50% of business will be in those markets by 2020. Acquisition of Daichi to Ranbaxy and Abbot by Piramals makes it clear that big pharma companies want to make a strong market presence in India.</div>
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“Rather than trying to find a use for approved medicines that were developed for a non-Asian phenotype, the move is to discover and develop medicines specifically to treat Asian diseases,” explains Paul Bolno, VP of Oncology R&D, Business Development at GSK. <a href="http://www.nature.com/nrd/journal/v9/n6/full/nrd3204.html">Here</a> is a Nature article </div>
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However, it will take a long time for the local doctors here in India to stop giving the pills without any label and any expiry dates on them. (pic; a local hospital gave me these medicines for a mild fever, you have to remember the tablets by its color).</div><div style="text-align: justify;"><br /></div>
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Shaji Varghesehttp://www.blogger.com/profile/00478370858361834571noreply@blogger.com0