Kinase Drug Discovery (eBook)

Dr Frederick W Goldberg is a Medicinal Chemist at AstraZeneca, UK. He received his MSci at Cambridge University, PhD at Imperial College London and a Postdoc (Fulbright scholarship) at the University of Texas at Austin. He has extensive experience of leading both chemistry and project teams within oncology, including targets that have delivered clinical candidates. He has over 30 published papers and patents, including a number of research papers and perspective articles on kinases. Dr Richard A Ward is a Computational Medicinal Chemist at AstraZeneca, UK. He received his BSc (Hons) in Chemistry with Bio-organic Chemistry at The University of Birmingham and gained a PhD in Computational Chemistry also at The University of Birmingham, under the supervision of Dr John Wilkie. He has extensive experience in target selection, lead generation and lead optimisation against kinase and non-kinase targets with a specialisation in covalent drug discovery. Along with publishing a number of papers on kinases, Richard is a co-inventor of the EGFR mutant kinase inhibitor osimertinib.

Introduction to Kinase Drug Discovery - Modern Approaches; New Screening Approaches for Kinases; The Screening and Design of Allosteric Kinase Inhibitors; Covalent Inhibition of Kinases; Small Molecule Macrocyclic Kinase Inhibitors; The Design of Brain Penetrant Kinase Inhibitors; Cutting Edge Approaches to Structure-based Computational Modelling of Kinases; The Properties of Kinase Inhibitors; Assessment and Optimisation of Kinases Inhibitor Selectivity to Achieve Candidates with an Appropriate Safety Profile; Drugging the Kinome; The Importance of Kinase Mutations in Cancer Drug Discovery; Kinase Inhibition for Immuno-oncology; A Structural Perspective of the Pseudokinome: Defining the Targetable Space; The Future of Kinase Therapeutics; Subject Index