Li / Stafford Kinase Inhibitor Drugs

1. Auflage 2011
ISBN: 978-1-118-21090-1
Verlag: John Wiley & Sons
Format: EPUB
Kopierschutz: Adobe DRM (»Systemvoraussetzungen)

E-Book, Englisch, 528 Seiten, E-Book

Reihe: Wiley series in drug discovery and development

A comprehensive resource on case studies of marketed kinasedrugs and promising drug trials
Since the discovery of protein kinase activity in 1954, thefield of protein kinase drug discovery has advanced dramatically.With the ongoing clinical success of the Bcr-Abl kinase inhibitorGleevec in the treatment of chronic myelogenous leukemia and sevenadditional marketed kinase inhibitor drugs, researchers havecompelling evidence that kinase inhibitors can be highlyefficacious in the treatment of diseases caused by aberrantactivity of protein kinase. Currently more than 100 protein kinaseinhibitors are in clinical development.
In one comprehensive volume, the editors, Dr. Rongshi Li and Dr.Jeffrey Stafford, present timely and important case studies ofmarketed kinase drugs and several of the most advanced kinaseinhibitors in clinical trials. Kinase Inhibitor Drugsincludes:
* Case studies from leading investigators and experts in the fieldthat provide firsthand accounts of kinase inhibitor discovery
* Current thinking on kinase structure, biochemistry, and signaltransduction pathways
* Information on state-of-the-art technologies and tools such asstructure-based and fragment-based drug discovery
* A lineup of clinical-phase growth factor receptor inhibitors
* Inhibitors of cell cycle kinases
* The discovery of allosteric inhibitors of MEK kinase
* Information on pharmacogenomics and its application to kinaseinhibitor clinical development

Autoren/Hrsg.

Li, Rongshi

Stafford, Jeffrey A.

Inhaltsverzeichnis

PREFACE.
CONTRIBUTORS.
PART I GROWTH FACTOR INHIBITORS: VEGFR2, ERBB2, AND OTHERKINASE.
1 Discovery and Development of Sunitinib (SU11248): AMultitarget Tyrosine Kinase Inhibitor of Tumor Growth, Survival,and Angiogenesis (Connie L. Sun, James G. Christensen, andGerald McMahon).
2 Tykerb Discovery: A Dual EGFR and ERBB2 Tyrosine KinaseInhibitor (Karen Lackey and G. Stuart Cockerill).
3 Discovery of Pazopanib: A Pan Vascular Endothelial GrowthFactor Kinase Inhibitor (Philip A. Harris and Jeffrey A.Stafford).
4 Road to ABT-869: A Multitargeted Receptor Tyrosine KinaseInhibitor (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 EndothelialGrowth 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 InhibitorQuest (Judith S. Sebolt-Leopold and Alexander J.Bridges).
9 Discovery of Allosteric MEK Inhibitors (Eli Wallaceand James F. Blake).
PART III CELL CYCLE KINASE INHIBITORS: AURORA KINASE AND PLKINHIBITORS.
10 Discovery of MK-0457 (VX-680) (Julian M. C.Golec).
11 Discovery of PHA-739358 (Daniele Fancelli and JürgenMoll).
12 Discovery of AZD1152: A Selective Inhibitor of Aurora-BKinase with Potent Antitumor Activity (Kevin M. Foote and AndrewA. 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 forthe Treatment of Cancer (Kevin W. Kuntz and Kyle A.Emmitte).
PART IV RELATED SPECIAL TOPICS.
15 Pharmacogenomics of Dasatinib (Sprycel) (Fei Huang andEdwin A. Clark).
16 Practical Use of Computational Chemistry in Kinase DrugDiscovery (James M. Veal).
17 Approaches to Kinase Homology Modeling: Successes andConsiderations for the Structural Kinome (Victoria A. Feher andJ. David Lawson).
18 Fragment-Based Drug Discovery of Kinase Inhibitors (DanielA. Erlanson).
19 Protein Kinase Structural Biology: Methods and Strategies forTargeted Drug Discovery (Clifford D. Mol, Kengo Okada, and DavidJ. Hosfield).
INDEX.

Über Autor(innen)

Rongshi Li, PhD, is an Associate Professor in the DrugDiscovery Department at H. Lee Moffitt Cancer Center and ResearchInstitute in Tampa, Florida.
Jeffrey A. Stafford, PhD, has led drug discovery researchat GlaxoSmithKline, Syrrx, and Takeda. He is a co-inventor of thetyrosine kinase inhibitor, pazopanib (Armala).