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.
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.
|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:||Birkbeck Schools and Departments > School of Science > Biological Sciences|
|Date Deposited:||14 Nov 2011 08:58|
|Last Modified:||17 Apr 2013 12:21|
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