Transforming fragments into candidates: small becomes big in medicinal chemistry
Fragment-based drug discovery (FBDD) represents a logical and efficient approach to lead discovery and optimisation. It can draw on structural, biophysical and biochemical data, incorporating a wide range of inputs, from precise mode-of-binding information on specific fragments to wider ranging phar...
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Published in | Drug discovery today Vol. 14; no. 13; pp. 630 - 646 |
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Main Authors | , , , |
Format | Journal Article |
Language | English |
Published |
Kidlington
Elsevier Ltd
01.07.2009
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | Fragment-based drug discovery (FBDD) represents a logical and efficient approach to lead discovery and optimisation. It can draw on structural, biophysical and biochemical data, incorporating a wide range of inputs, from precise mode-of-binding information on specific fragments to wider ranging pharmacophoric screening surveys using traditional HTS approaches. It is truly an enabling technology for the imaginative medicinal chemist. In this review, we analyse a representative set of 23 published FBDD studies that describe how low molecular weight fragments are being identified and efficiently transformed into higher molecular weight drug candidates. FBDD is now becoming warmly endorsed by industry as well as academia and the focus on small interacting molecules is making a big scientific impact.
Unlocking medicinal chemistry innovation with FBDD strategies. |
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Bibliography: | ObjectType-Article-2 SourceType-Scholarly Journals-1 ObjectType-Feature-3 content type line 23 ObjectType-Review-1 |
ISSN: | 1359-6446 1878-5832 |
DOI: | 10.1016/j.drudis.2009.03.009 |