Twenty years on: the impact of fragments on drug discovery

Daniel A. Erlanson; Stephen W. Fesik; Roderick E. Hubbard; Wolfgang Jahnke; Harren Jhoti

doi:10.1038/nrd.2016.109

Twenty years on: the impact of fragments on drug discovery

Daniel A. Erlanson^*, Stephen W. Fesik, Roderick E. Hubbard, Wolfgang Jahnke, Harren Jhoti

^*Corresponding author for this work

Chemistry

Research output: Contribution to journal › Review article › peer-review

Abstract

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.

Original language	English
Pages (from-to)	605-619
Number of pages	15
Journal	Nature Reviews Drug Discovery
Volume	15
Issue number	9
Early online date	15 Jul 2016
DOIs	https://doi.org/10.1038/nrd.2016.109
Publication status	Published - Sept 2016

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10.1038/nrd.2016.109

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abstract = "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.",

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Twenty years on: the impact of fragments on drug discovery

Abstract

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