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Twenty years on: the impact of fragments on drug discovery

Jahnke, Wolfgang, Erlanson, Daniel A, Fesik, Stephen W, Hubbard, Roderick E and Jhoti, Harren (2016) Twenty years on: the impact of fragments on drug discovery. Nature Reviews Drug Discovery, 1 (1). pp. 1-2. ISSN 1474-17761474-1784


After twenty years of sometimes quiet growth, fragment-based drug discovery (FBDD) has become mainstream. More than 30 drug candidates derived from fragments have entered the clinic, with one approved and several more in advanced trials. FBDD has been widely applied in both academia and industry, as evidenced by the large number of papers from universities, non-profit research institutions, biotechs, and pharmaceutical companies. Moreover, FBDD draws on a diverse range of disciplines, from biochemistry and biophysics to computational and medicinal chemistry. As the promise of FBDD strategies becomes increasingly realized, now is an opportune time to draw lessons and point the way to the future. This review briefly discusses how to design fragment libraries, how to select screening techniques, and how to make the most of information gleaned from them. It also shows how concepts from FBDD have permeated and enhanced drug discovery efforts.

Item Type: Article
Date Deposited: 12 Aug 2016 00:45
Last Modified: 12 Aug 2016 00:45