Current Challenges in Fragment Based Drug Discovery

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May 11, 2012

Rod Hubbard, Professor, University of York

Abstract
The past ten years has seen tremendous developments in the experimental methods of “Fragment-Based Lead Discovery”, FBLD, with many compounds now in clinical trials and the first compound now on the market. The central feature is that the drug discovery process begins with identification of small (<250 MW), weakly binding (affinity of 100s of μM) compounds which are then optimised to drug candidates by structure-guided design. The advantages are that a small library can sample a potentially large chemical diversity to generate novel lead compounds and that hits can be identified for new classes of target for which existing compound collections cannot provide a hit. This presentation will review the current status of the methods and their application and survey the current issues: -deciding which fragments to progress - between 10-200 chemically diverse fragments can be found as hits from screening 1200 fragments - which fragments should be progressed? -how to work with challenging targets, such as protein-protein interactions -how important is the fragment library?

Drug Discovery

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