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Targeting cancer using fragment based drug discovery

Turnbull, Andrew P. and Boyd, S.M. (2011) Targeting cancer using fragment based drug discovery. Anticancer Agents In Medicinal Chemistry 12 (1), pp. 40-48. ISSN 1871-5206.

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Official URL: http://www.benthamdirect.org/pages/b_viewarticle.p...

Abstract

Over the past decade, fragment-based drug discovery has developed significantly and has gained increasing popularity in the pharmaceutical industry as a powerful alternative and complement to traditional high-throughput screening approaches for hit identification. Fragment-based methods are capable of rapidly identifying starting points for structure-based drug design from relatively small libraries of low molecular weight compounds. The main constraints are the need for sensitive methods that can reliably detect the typically weak interactions between fragments and the target protein and strategies for transforming fragments into higher molecular weight drug candidates. This approach has recently been validated as series of compounds from various programs have entered clinical trials.

Item Type: Article
Keyword(s) / Subject(s): Fragment screening, Ligand efficiency, Drug discovery, Cancer, high-throughput screening (HTS), Crystallography, fluorimetry, Phosphoinositide-Dependent Kinase-1 (PDK1), Anti-cancer, Cyclindependent kinase (CDK)
School or Research Centre: Birkbeck Schools and Research Centres > School of Science > Biological Sciences
Depositing User: Administrator
Date Deposited: 14 Nov 2011 08:58
Last Modified: 17 Apr 2013 12:21
URI: http://eprints.bbk.ac.uk/id/eprint/4364

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