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Nat Rev Drug Discov. 2016 Sep;15(9):605-619. doi: 10.1038/nrd.2016.109. Epub 2016 Jul 15.

Twenty years on: the impact of fragments on drug discovery.

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Carmot Therapeutics, Inc. 409 Illinois Street, San Francisco, California 94158, USA.
Department of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, USA.
York Structural Biology Laboratory, Department of Chemistry, University of York, York YO10 5DD, UK.
Vernalis Research, Granta Park, Abington, Cambridge CB21 6GB, UK.
Novartis Institutes for Biomedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Astex Pharmaceuticals, 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA, UK.


After 20 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 two 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, biotechnology companies 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.

[Indexed for MEDLINE]

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