Recent Developments in Fragment-Based Drug Discovery

Miles Congreve is Director of Chemistry at Astex Therapeutics in Cambridge, U.K., where he is responsible for the company’s fragment screening collection and for its hits to leads chemistry function. He joined Astex in 2001. He previously held various positions at GlaxoSmithKline (1993−2001), working on a broad range of medicinal chemistry and hits to leads projects at Ware and then Stevenage before moving to Cambridge in 1999 to run the GlaxoWellcome chemistry research facility embedded in the University of Cambridge chemistry department. His Ph.D. studies were also carried out at the University of Cambridge (1990−1993), supervised by Professor Andrew Holmes.

Gianni Chessari is a Senior Computational Chemist at Astex Therapeutics, joining the company in 2002. He has been involved in the construction of the fragment corporate libraries and also contributed to the design of inhibitors for a number of drug targets including thrombin, β-secretase, urokinase, and Hsp90. Before working at Astex, he carried out postdoctoral research at the Institute of Cancer Research in London (U.K.) and the CNRS in Lille (France). He received his Ph.D. in Organic Chemistry at the University of Sheffield (U.K.) in 2000 under the supervision of Professor Christopher Hunter.

Dominic Tisi is a Senior Structural Biologist working in the Protein Structure group at Astex Therapeutics. Joining the company in 2000, he has worked on several drug discovery projects including JAK2, Aurora kinase, and PTP1B, performing fragment screens using X-ray crystallography. He received his Ph.D. in Protein Crystallography from Birkbeck College, London, and GlaxoWellcome, Stevenage, in 1998 before carrying out postdoctoral research at Imperial College, London, prior to joining Astex Therapeutics.

Andrew J. Woodhead is a Senior Chemist at Astex Therapeutics. He has been with Astex since 2001 and has experience in fragment hit identification and structure based drug design for a number of targets including the oncology targets CDK2 and HSP90. He began his medicinal chemistry career with Wyeth in 1992, working on CNS disorders such as migraine and depression. In 1994 he joined Roche to focus initially on inflammatory diseases and then moved to the virology department before finally joining the lead generation chemistry group. He carried out his academic studies at De Montfort University, Leicester, U.K.