Tuesday, April 19, 2011

Enoyl reductase: One target, Two major Global Threats

Tuberculosis and Malaria are two major global threats both account 5 million deaths annually (mostly in poor 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 resistance has developed or is developing to existing therapy. Scientists around the world are seeking new ways to combat the two opportunistic pathogens.
Mycobacterium tuberculosis and Plasmodium Falciparum responsible both organisms share enzymatic components of the type II fatty acid biosynthetic pathway (FAS-II). Enoyl acyl carrier protein reductase (ENR), is one of the key type II enzyme, has been repeatedly validated as an effective antimicrobial target (eg INH, diazoborines , triclosan , and thiolactomycin)

Triclosan, the ENR inhibitor showed very good activity against both organisms. Targeting ENR with new class of compounds may yield new Drug for the use against these devastating pathogens.

Tuesday, March 29, 2011

The Future of Drug Discovery

 The new technologies promise to fill drug development pipeline with small molecule candidates is unfulfilled, so pharmaceutical industry is currently undergoing rapid changes, they are moving aggressively into large molecule drug development.
"Drug space” that is not part of the current drug development includes non-Lipinski NCEs, nanomedicines, nucleic acid-based drugs etc will include in future. One of the major challenges for medicinal chemist is to find small molecule inhibitors for protein-protein interactions.