Thursday, August 16, 2012
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Crystal structures of HCV NS3/4A protease complex
with HCV protease inhibitors
Crystal structures of HCV
NS3/4A proteases complexed with HCV protease inhibitors could aid the
development of new therapeutics against drug-resistant HCV strains.
Researchers generated crystal structures of wild-type HCV NS3/4A protease and
three common drug-resistant variants in complex with four small molecule
protease inhibitors. The structures showed that Incivek telaprevir, danoprevir,
vaniprevir and MK-5172 interact at sites
on the wild-type protease that are mutated in drug-resistant variants, such
as R155, A156 and D168. Next steps include characterizing additional
drug-resistant variants of the HCV NS3/4A protease complex and conducting
studies to better understand the role of the protease's helicase domain.
Vertex Pharmaceuticals Inc.,
Johnson & Johnson and
Mitsubishi Tanabe Pharma Corp.
market Incivek to treat HCV.
Merck & Co. Inc.'s
vaniprevir is in Phase III testing and MK-5172 is in Phase II testing for
Roche's danoprevir is in
Phase II testing to treat HCV.
SciBX 5(32); doi:10.1038/scibx.2012.853
Published online Aug. 16, 2012
status not applicable; available for partnering and collaborations
Romano, K.P. et al. PLoS Pathog.; published online July 26, 2012;
Contact: Celia A. Schiffer, University of Massachusetts
Medical School, Worcester, Mass.
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