Astex Scientists Publish The Discovery Of Novel Allosteric Modulators For The Key Therapeutic Targets HCV NS3 And PKM2 In Nature Journals
DUBLIN, Calif., Oct. 15, 2012 (GLOBE NEWSWIRE) -- Astex Pharmaceuticals, Inc. (Nasdaq:ASTX), a pharmaceutical company dedicated to the discovery and development of novel small molecule therapeutics, announced that Astex scientists have published two new articles describing the discovery of novel allosteric modulators for the key therapeutic targets HCV NS3 and PKM2 in Nature Journals.
Astex Pharmaceuticals used the company's leading fragment-based drug discovery platform, Pyramid™, to identify, in two separate studies, new allosteric pockets on the HCV NS3 protein and the PKM2 protein involved in tumor metabolism. The study on HCV NS3 which has just been published in Nature Chemical Biology 1 highlights the discovery of a novel allosteric pocket situated between the protease and helicase domains of the NS3 protein. It also describes how Astex scientists exploited this pocket to develop novel, first-in-class inhibitors of the HCV NS3 protein that interact with both the protease and helicase domains. A drug candidate from this program is due to enter clinical trials during 2013.
In the second study, now published in Nature 2, the Pyramid platform was used to identify a novel allosteric pocket on the tumor metabolism target PKM2 and unravel the role of serine on the function of this key cancer target. This novel allosteric pocket provides a new opportunity to discover allosteric modulators of PKM2 that could be developed into anti-cancer agents.Dr. Harren Jhoti, president and director of Astex Pharmaceuticals, commented, "These two studies published in the leading Nature Journals underline the preeminent position Astex retains in using fragment-based drug discovery to identify novel drug candidates against technically challenging targets. We continue to develop the fragment-discovery platform to address more intractable drug targets, not only allosteric pockets but also protein-protein interactions, in our drive to develop new medicines for patients." About Astex Pharmaceuticals Astex Pharmaceuticals is dedicated to the discovery and development of novel small molecule therapeutics with a focus on oncology. The Company is developing a proprietary pipeline of novel therapies and is creating de-risked products for partnership with leading pharmaceutical companies. Astex Pharmaceuticals co-developed DACOGEN® (decitabine) for Injection and receives significant royalties on global sales from Eisai in North America and from Janssen-Cilag in the rest of the world.
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