Thursday, October 11, 2012
Publication and contact
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.
All contents Copyright © 1993-2017 BioCentury Publications, Inc. ALL RIGHTS RESERVED. All use of this Web Site and its contents is governed by the BioCentury User Agreement
. The contents of this Web Site are protected under U.S. and foreign copyright and intellectual property laws, and no part of this Web Site or its contents may be photocopied, reproduced or retransmitted in any form without the written consent of BioCentury, which may be requested from Reprints/Permissions
. BioCentury®; The Bernstein Report on BioBusiness™; The BioCentury 100™; The Clear Route to ROI™; Because Real Intelligence is Hard to Find™; BCIQ™; and BioPharma's Knowledge Center™; are trademarks of BioCentury Publications, Inc., P.O. Box 1246, San Carlos, CA 94070. SciBX® and SciBX: Science-Business eXchange® are trademarks of Nature America, Inc. that are jointly used by BioCentury Publications, Inc. and Nature America, Inc.
Thanks for purchasing this article.
Please bookmark this url for future reference.
We have also sent you a confirming e-mail with a receipt and this same url for your
close [ X ]