Journal
CURRENT OPINION IN STRUCTURAL BIOLOGY
Volume 20, Issue 4, Pages 497-507Publisher
CURRENT BIOLOGY LTD
DOI: 10.1016/j.sbi.2010.04.003
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Fragment-based ligand screening is now established as an emerging paradigm for drug discovery. Here we examine the recent literature looking at how structural biology has been used in a variety of successful fragment-screening applications. We argue that the determination of experimental binding modes has proved to be one of the mainstays of successful fragment-based approaches and that this reflects the difficulty in optimising a fragment to a lead molecule in the absence of structural information. We focus on antimicrobial research where fragment-based drug discovery allows control of the physical properties of the emerging lead molecule.
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