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Targeting Cancer Using Fragment Based Drug Discovery

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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.





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Keywords: Anti-cancer; Cancer; Crystallography; Cyclindependent kinase (CDK); Drug discovery; Fragment screening; Ligand efficiency; Phosphoinositide-Dependent Kinase-1 (PDK1); fluorimetry; high-throughput screening (HTS)

Document Type: Research Article

Publication date: 01 January 2012

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