Targeting Cancer Using Fragment Based Drug Discovery

Title: Targeting Cancer Using Fragment Based Drug Discovery

Volume: 12 Issue: 1

Author(s): Andrew P. Turnbull and Susan M. Boyd

Affiliation:

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

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.

Cite this article as:

P. Turnbull Andrew and M. Boyd Susan, Targeting Cancer Using Fragment Based Drug Discovery, Anti-Cancer Agents in Medicinal Chemistry 2012; 12 (1) . https://dx.doi.org/10.2174/187152012798764660