Kinase inhibition remains an area of significant interest, and growing importance, across academia and the pharmaceutical industry. There are now many marketed drugs that target kinases and a significant number of compounds are currently in various stages of clinical development. This book is a forward-looking analysis of a number of key areas for kinase inhibition in the coming years and builds on the first volume. This includes topics such as screening approaches to target kinases along with different modes of inhibition such as allosteric and covalent. Novel approaches such as macrocyclisation are considered along with how the properties of kinase inhibitors have evolved, including the potential for brain penetration. Recent areas of great importance also covered include cutting edge molecular modelling approaches and the importance of kinase mutations. The evolving biology of kinases has also resulted in increased interest in the immuno-oncology area and also pseudokinases as a target family. As with the first volume the book finishes with a forward looking view of how research against this fascinating target class may evolve.
Cuprins
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
Despre autor
Dr Frederick W Goldberg is a Medicinal Chemist at Astra Zeneca, UK. He received his MSci at Cambridge University, Ph D 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 Astra Zeneca, UK. He received his BSc (Hons) in Chemistry with Bio-organic Chemistry at The University of Birmingham and gained a Ph D 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.
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