Emerging opportunities and challenges in target directed cancer drug discovery - Rob Van Montfort

Emerging opportunities and challenges in target-directed cancer drug discovery - Rob van Montfort Centre for Cancer Drug Discovery, Divisions of Cancer Therapeutics and Structural Biology, The Institute of Cancer Research, London, SM2 5GP, UK. Rob.vanmontfort@icr.ac.uk In this talk I will briefly introduce the Centre for Cancer Drug Discovery (CCDD), the Centre for Target Validation (CTV), and the Centre for Protein Degradation (CPD) at ICR. In the main body of the talk, I will talk about the multi-faceted orthogonal approaches we use in hit identification and compound optimisation in the small molecule drug discovery programmes at CCDD. I will describe how we combine Virtual Screening and biochemical HTS campaigns with biophysical and crystallographic fragment screening and how we integrate these efforts with structural biology techniques such as X-ray crystallography and cryo-electron microscopy to discover potent and selective inhibitors and degraders of promising cancer targets. I will use examples from the academic drug discovery at the ICR and will briefly discuss how we use Alphafold in our research.