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  Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 12 Issue 1
ISSN: 1871-5206

 
   All Titles

Targeting Cancer Using Fragment Based Drug Discovery
pp.40-48 (9) Authors: Andrew P. Turnbull, Susan M. Boyd
 
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.

Keywords: Fragment screening, Ligand efficiency, Drug discovery, Cancer, high-throughput screening (HTS), Crystallography, fluorimetry, Phosphoinositide-Dependent Kinase-1 (PDK1), Anti-cancer, Cyclindependent kinase (CDK)
Affiliation: CRT Discovery Laboratories, Department of Crystallography, Birkbeck College, University of London, Malet Street, London, WC1E 7HX.

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