Thursday, October 11, 2012
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HCV NS3/4A protein complex
using crystals of the HCV NS3/4A holoenzyme identified inhibitors of an
allosteric site that could help treat HCV infection. Structure-guided
optimization of a lead fragment against an allosteric site on the HCV NS3/4A
holoenzyme yielded a compound that inhibited the enzyme with an IC50
under 10 nM. In a cell-based assay, the optimized compound showed antiviral
activity with an EC50 of 8.3 nM. IND-enabling studies of an
optimized molecule that binds the same site are ongoing.
Pharmaceuticals Inc.'s lead HCV NS3/4A protease inhibitor,
which is the optimized molecule, is in preclinical development to treat HCV
Pharmaceuticals Inc. markets Incivek
a small molecule HCV NS3/4A protease inhibitor, to treat HCV infection.
& Co. Inc. markets Victrelis
a small molecule HCV NS3/4A protease inhibitor, for the same indication.
At least six other companies have inhibitors of the HCV NS3/4A protease in
Phase III testing or earlier to treat HCV infection (see Closing time for HCV
protease, page 6).
SciBX 5(40); doi:10.1038/scibx.2012.1055
Published online Oct. 11, 2012
Patent applications filed
covering composition of matter; available for licensing and partnering
Saalau-Bethell, S.M. et
al. Nat. Chem. Biol.; published online Sept. 30, 2012;
Contact: Harren Jhoti,
Astex Pharmaceuticals Inc., Cambridge, U.K.
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