Fragment-Based Screening and Structure-Based Design at ICR: Discovering High Quality Leads in Cancer Drug Discovery

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SELECTBIO

Rob Van Montfort, Leader, Hit Discovery and Structural Design Unit, Institute of Cancer Research

Abstract
The CRUK Cancer Therapeutics Unit at the Institute of Cancer Research is a multidisciplinary 'bench to bedside' unit dedicated to the discovery and development of novel therapeutics for the treatment of cancer. With the establishment of high-throughput X-ray crystallography, fragment screening and biophysical technologies such as thermal denaturation assays, surface plasmon resonance, and isothermal titration calorimetry the unit has significantly enhanced its hit discovery strategy. Further integration of fragment-based screening with the Unit's existing assay development and high-throughput screening capabilities has created a flexible and state-of-the-art academic hit discovery operation. In this presentation the impact of the implementation, and development of fragment screening and its combination with high throughput screening will be discussed using examples from our portfolio including the checkpoint kinases CHK1 and CHK2, which are of extensive interest as potential targets for anti-cancer therapies.