Kinase Drug Discovery

This is the first book to examine the future opportunities and challenges in the development of drugs which target kinases 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. Kinase drug discovery remains an area of significant interest across academia and in the pharmaceutical industry. There are now around 13 FDA approved small molecule drugs which target kinases and many more compounds in various stages of clinical development. Although there have been a number of reviews/publications on kinase research, this book fills a gap in the literature by considering the current and future opportunities and challenges in targeting this important family of enzymes. The book is forward-looking and identifies a number of hot topics and key areas for kinase drug discovery over the coming years. It includes contributions from highly respected authors with a combined experience in the industry of well over 200 years, which has resulted in a book of great interest to the kinase field and across drug discovery more generally. Readers will gain a real insight into the huge challenges and opportunities which this target class has presented drug discovery scientists. The many chapters cover a wide breadth of topics, are well written and include high quality colour and black and white images. Topics covered include an outline of how medicinal chemistry has been able to specifically exploit this unique target class, along with reflections on the mechanisms of kinases inhibitors. Also covered is resistance to kinase inhibitors caused by amino acid mutations, case studies of kinase programs and reviews areas beyond protein kinases and beyond the human kinome. Also described are modern approaches to finding kinase leads and the book finishes with a reflection of how kinase drug discovery may progress over the coming years.