Astex scientists describe novel HSP90 inhibitors in two key publications in Journal of Medicinal Chemistry

Astex scientists describe novel HSP90 inhibitors in two key publications in Journal of Medicinal Chemistry Cambridge, UK, 29th July 2010. Astex Therapeutics, the UK-based biotechnology company developing targeted therapies for oncology and virology, announced today that two key papers detailing its fragment -based drug discovery approach to heat shock protein 90 (HSP90) inhibitors have been published back -to-back in the industry -leading Journal of Medicinal Chemistry*. The first paper describes fragment -based screening of HSP90 and subsequent structure -guided chemistry that improved the affinity of the initial lead compounds by over a million -fold with the addition of only 6 atoms. The companion paper describes how the lead compound was optimised into the clinical candidate, AT13387, a potentially best -in-class HSP90 inhibitor which is entering into Phase II clinical trials for the treatment of a variety of cancers. Together, the papers demonstrate the efficiency with which the Company’s fragment-based drug discovery platform, Pyramid™, can be used to identify small molecule drugs. -ends- Contact Jeremy Carmichael, PhD Director of Business Development Astex Therapeutics Ltd 436 Cambridge Science Park Milton Road, Cambridge CB4 0QA, UK Tel: +44(0)1223 226200 Fax: +44(0)1223 226201 [email protected] www.astex-therapeutics.com * Publication References Woodhead et al. Discovery of (2,4 -Dihydroxy-5-isopropylphenyl) -[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl] methanone (AT13387), a Novel Inhibitor of the Molecular Chaperone Hsp90 by Fragment Based Drug Design. J. Med. Chem. (DOI: 10.1021/jm100060b) Published online July 28 2010 Murray et al. Fragment -Based Drug Discovery Applied to HSP90. Discovery of Two Lead Series with High Ligand Efficiency. J. Med. Chem. (DOI: 10.1021/jm100059d) Published online July 27 2010 About Astex Therapeutics Astex is a UK-based biotechnology company that discovers and develops novel small molecule therapeutics. Using its pioneering fragment -based drug discovery platform Pyramid™, Astex has built a pipeline of five molecularly -targeted oncology drugs, of which three are currently being tested in clinical trials and two are in pre -clinical development. In addition to its proprietary research programmes, Astex ’s productivity in lead discovery has been endorsed through numerous partnerships with major pharmaceutical companies, including AstraZeneca, Bayer -Schering, Boehringer Ingelheim, GlaxoSmithKline, Novartis and Johnson & Johnson. For further information on Astex please visit the Company ’s website at www.astex-therapeutics.com

The release as fetched from its publisher. astx.com ↗