Kinase drug discovery remains an area of significant interest across the pharmaceutical industry and academia. There are currently 13 FDA-approved small molecule drugs and over 500 small molecules in active development targeting kinases. These agents have delivered significant benefits to patients that can be measured in life extension or improvement in the quality of life in diseases like cancer and inflammation. The kinase family has therefore been a rich source of new targets and opportunities for the pharmaceutical industry but has also presented significant and unique challenges. Although there have been a number of books on kinase research, this book focuses on the future opportunities and challenges, rather than on case studies of specific targets. The editors have also aimed to cover broad themes on a number of hot topics in current kinase drug discovery. Highly respected authors in the field have been identified with a combined drug discovery experience of over 200 years. Areas covered include an insight into how medicinal chemistry has been able to exploit this unique target class, along with reflections on the varied mechanisms of kinase inhibitors. Also addressed is resistance to kinase inhibition caused by amino acid mutations, non-protein kinases and applications beyond the human kinome into parasitic diseases. Modern approaches to finding kinase leads and reflections on how the field may progress over coming years are also described. This book will be of great interest to pharmaceutical scientists, biologists and medicinal chemists working in drug discovery and drug development.

Dr Richard A Ward is a Computational Chemist, Oncology iMed, 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. His experience is in target selection, lead identification, lead generation and lead optimisation against kinase and non-kinase targets with specialisations in fragment-based lead generation along with library design and collection enhancement activities. He has publications in lead generation, virtual screening, druggability assessments, collection enhancement activities using computational ring enumeration along with reagent enhancement and has published supporting papers with a biological focus. He is also named as an inventor on a number of small molecule patents. Dr Frederick W Goldberg is a Medicinal Chemist at AstraZeneca, UK. He received his MSci (Hons) in Natural Sciences (Chemistry) at Cambridge University and then gained a PhD in Organic Chemistry at Imperial College, London, under the supervision of Dr Alan Armstrong. Subsequently he completed a Postdoc (AstraZeneca Fulbright scholarship) at the University of Texas at Austin, USA on "Formal synthesis of Diazonamide A", under the supervision of Dr Philip Magnus. He is presently a lead chemist on various kinase and non-kinase targets, working within the oncology lead generation group and diabetes lead optimization groups. He has publications in kinase lead generation and has filed 8 patents as primary inventor.

An Introduction to Kinase Inhibition; The Kinome and its Impact on Medicinal Chemistry; Contemporary Approaches to Kinase Lead Generation; The Learning and Evolution of Medicinal Chemistry against Kinase Targets; The Mechanism and Kinetics of Kinase Inhibitors; Kinase mutations and resistance in cancer; Non-Protein Kinases as Therapeutic Targets; The Drug Discovery and Development of Kinase Inhibitors Outside of Oncology; Allosteric Activators of Glucokinase (GK) for the Treatment of Type 2 Diabetes; Drug Discovery and Non-Human Kinomes; The future of kinase drug discovery