Kinase Inhibitor Drugs covers a wide and comprehensive range of topics about kinase-targeted inhibitors in cancer therapy, one of the hottest drug targets in modern drug discovery. It brings together and summarizes important information and advances in the field to allow researchers and drug discoverers to easily discern the state of targeted cancer drug discovery. Complete with case studies of approved kinase inhibitors or those in late-phase clinical trials for cancer therapy, this is an ideal reference for pharmaceutical scientists developing small molecule and biotech drugs to treat cancer.
Rongshi Li, PhD , is an Associate Professor in the Drug Discovery Department at H. Lee Moffitt Cancer Center and Research Institute in Tampa, Florida. Jeffrey A. Stafford, PhD , has led drug discovery research at GlaxoSmithKline, Syrrx, and Takeda. He is a co-inventor of the tyrosine kinase inhibitor, pazopanib (Armala).
PREFACE. CONTRIBUTORS. PART I GROWTH FACTOR INHIBITORS: VEGFR2, ERBB2, AND OTHER KINASE. 1 Discovery and Development of Sunitinib (SU11248): A Multitarget Tyrosine Kinase Inhibitor of Tumor Growth, Survival, and Angiogenesis ( Connie L. Sun, James G. Christensen, and Gerald McMahon ). 2 Tykerb Discovery: A Dual EGFR and ERBB2 Tyrosine Kinase Inhibitor ( Karen Lackey and G. Stuart Cockerill ). 3 Discovery of Pazopanib: A Pan Vascular Endothelial Growth Factor Kinase Inhibitor ( Philip A. Harris and Jeffrey A. Stafford ). 4 Road to ABT-869: A Multitargeted Receptor Tyrosine Kinase Inhibitor ( Michael Michaelides and Daniel H. Albert ). 5 Discovery of Motesanib ( Andrew S. Tasker and Vinod F. Patel ). 6 Discovery of Brivanib Alaninate: A Dual Vascular Endothelial Growth Factor and Fibroblast Growth Factor Receptor Inhibitor ( Rajeev S. Bhide and Joseph Fargnoli ). 7 S tructure-Based Design and Characterization of Axitinib ( Robert S. Kania ). PART II GROWTH FACTOR INHIBITORS: MEK INHIBITORS. 8 Road to PD0325901 and Beyond: The MEK Inhibitor Quest ( Judith S. Sebolt-Leopold and Alexander J. Bridges ). 9 Discovery of Allosteric MEK Inhibitors ( Eli Wallace and James F. Blake ). PART III CELL CYCLE KINASE INHIBITORS: AURORA KINASE AND PLK INHIBITORS. 10 Discovery of MK-0457 (VX-680) ( Julian M. C. Golec ). 11 Discovery of PHA-739358 ( Daniele Fancelli and Jurgen Moll ). 12 Discovery of AZD1152: A Selective Inhibitor of Aurora-B Kinase with Potent Antitumor Activity ( Kevin M. Foote and Andrew A. Mortlock ). 13 Case Study of Aurora-A Inhibitor MLN8054 ( Christopher F. Claiborne and Mark G. Manfredi ). 14 Discovery of GSK461364: A Polo-like Kinase 1 Inhibitor for the Treatment of Cancer ( Kevin W. Kuntz and Kyle A. Emmitte ). PART IV RELATED SPECIAL TOPICS. 15 Pharmacogenomics of Dasatinib (Sprycel) ( Fei Huang and Edwin A. Clark ). 16 Practical Use of Computational Chemistry in Kinase Drug Discovery ( James M. Veal ). 17 Approaches to Kinase Homology Modeling: Successes and Considerations for the Structural Kinome ( Victoria A. Feher and J. David Lawson ). 18 Fragment-Based Drug Discovery of Kinase Inhibitors ( Daniel A. Erlanson ). 19 Protein Kinase Structural Biology: Methods and Strategies for Targeted Drug Discovery ( Clifford D. Mol, Kengo Okada, and David J. Hosfield ). INDEX.
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