Protein Kinases as Drug Targets (Methods and Principles in Medicinal Chemistry 49)

This timely guide to kinase inhibitor drug discovery is the first to cover the entire drug pipeline, from target identification to compound development and clinical application. Edited by pioneers in the field, on the drug development side this ready reference discusses classical medicinal chemistry approaches as well as current chemical genomics strategies. On the clinical side, both current and future therapeutic application areas for kinase inhibitor drugs are addressed, with a strong focus on oncology drugs.Backed by recent clinical experience with first-generation drugs in the battle against various forms of cancer, this is crucial reading for medicinal, pharmaceutical and biochemists, molecular biologists, and oncologists, as well as those working in the pharmaceutical industry. Cover......Page 1 Frontmatter......Page 2 Copyright page......Page 5 Contents......Page 6 List of Contributors......Page 12 Preface......Page 16 A Personal Foreword......Page 18 Part One - Hit Finding and Profiling for Protein Kinases: Assay Development and Screening, Libraries......Page 23 1: In Vitro Characterization of Small-Molecule Kinase Inhibitors......Page 25 2: Screening for Kinase Inhibitors: From Biochemical to Cellular Assays......Page 67 3: Dissecting Phosphorylation Networks: The Use of Analogue-Sensitive Kinases and More Specific Kinase Inhibitors as Tools......Page 91 Part Two - Medicinal Chemistry......Page 107 4: Rational Drug Design of Kinase Inhibitors for Signal Transduction Therapy......Page 109 5: Kinase Inhibitors in Signal Transduction Therapy......Page 137 6: Design Principles of Deep Pocket-Targeting Protein Kinase Inhibitors......Page 167 7: From Discovery to Clinic: Aurora Kinase Inhibitors as Novel Treatments for Cancer......Page 217 Part Three - Application of Kinase Inhibitors to Therapeutic Indication Areas......Page 251 8: Discovery and Design of Protein Kinase Inhibitors: Targeting the Cell cycle in Oncology......Page 253 9: Medicinal Chemistry Approaches for the Inhibition of the p38 MAPK Pathway......Page 293 10: Cellular Protein Kinases as Antiviral Targets......Page 327 11: Prospects for TB Therapeutics Targeting Mycobacterium tuberculosis Phosphosignaling Networks......Page 371 Index......Page 387 In vitro characterization of small-molecule kinase inhibitors Screening for kinase inhibitors: from biochemical to cellular assays Dissecting phosphorylation networks: the use of analogue-sensitive kinases and more specific kinase inhibitors as tools Rational drug design of kinase inhibitors for signal transduction therapy Kinaes inhibitors in signal transduction therapy Design principles of deep pocket-targeting protein kinase inhibitors From discovery to clinic: aurora kinase inhibitors as novel treatments for cancer Discovery and design of protein kinase inhibitors: targeting the cell cycle in oncology Medicinal chemistry approaches for the inhibition of the p38 MAPK pathway Cellular protein kinases as antiviral targets Prospects for TB therapeutics targeting mycobacterium tuberculosis phosphosignaling networks.

This timely guide to kinase inhibitor drug development is the first to cover the entire drug pipeline, from target identification to compound development and clinical application. Edited by the pioneers in the field, on the drug development side this ready reference discusses classical medicinal chemistry approaches as well as current chemical genomics strategies. On the clinical side, both current and future therapeutic application areas for kinase inhibitor drugs are addressed, with a strong focus on oncology drugs.
Backed by recent clinical experience with first-generation drugs in the battle against various forms of cancer, this is crucial reading for medicinal, pharmaceutical and biochemists, molecular biologists, and oncologists, as well as those working in the pharmaceutical industry.

With kinase inhibitors being widely seen as the long-sought 'magic bullet' to conquer cancer, this comprehensive guide to kinase inhibitor drug development covers the entire drug pipeline, from target identification to compound development and clinical application Kinase inhibitors are widely seen as the long-sought 'magic bullet' to conquer cancer. Here, current strategies for kinase drug development are presented, backed by recent clinical experience from first-generation drugs against various forms of cancer.