Current Perspectives in Fragment Based Ligand Discovery



July 21, 2011

The past ten years has seen tremendous developments in the experimental methods of “Fragment-Based Lead Discovery”, FBLD. 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. The main challenges are design of the library, robust identification of which fragments bind and the need for structural information to decide how and which fragments to progress. This presentation will review the current status of the methods and their applications. Current issues like the following will also be discussed; library design (how many compounds, what size compounds?), deciding which fragments to progress and how to work with challenging targets, such as protein-protein interactions.

Drug Discovery

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