Protein Tyrosine Kinases

Leading researchers, from the Novartis group that pioneered Gleevec/Gliveca and around the world, comprehensively survey the state of the art in the drug discovery processes (bio- and chemoinformatics, structural biology, profiling, generation of resistance, etc.) aimed at generating PTK inhibitors for the treatment of various diseases, including cancer. Highlights include a discussion of the rationale and the progress made towards generating "selective" low molecular-weight kinase inhibitors; an analysis of the normal function, role in disease, and application of platelet-derived growth factor antagonists; and a summary of the factors involved in successful structure-based drug design. Additional chapters address the advantages and disadvantages of in vivo preclinical models for testing protein kinase inhibitors with antitumor activity and the utility of different methods in the drug discovery and development process for determining "on-target" vs "off-target" effects of kinase inhibitors.

ISBN 158829384X   Pages 308 ISBN13 9781588293848 (What's this?)   Volumes 1 Publisher Humana Press Inc.   Weight (grammes) 609 Imprint Humana Press Inc.   Published in Totowa, NJ Format Hardback   Series title Cancer Drug Discovery & Development Publication date 01 Sep 2005   Height (mm) 234 Library of Congress 2005006248   Width (mm) 156 DEWEY 572.769   Spine width (mm) 19 DEWEY edition DC22   Academic level Professional / Scholarly

1		Protein tyrosine kinases as targets for cancer and other indications by Mark Pearson and Carlos Garcia-Echeverria and Doriano Fabbro		1
2		Inhibitors of signaling interfaces : targeting Src homology 2 domains in drug discovery by Carlos Garcia-Echeverria		31
3		PI3-kinase inhibition : a target for therapeutic intervention by Peter M. Finan and Stephen G. Ward		53
4		Src as a target for pharmaceutical intervention : potential and limitations by Mira Susa and Martin Missbach and Rainer Gamse and Michaela Kneissel and Thomas Buhl and Jurg A. Gasser and Markus Glatt and Terence O'Reilly and Anna Teti and Jonathan Green		71
5		Activated FLT3 receptor tyrosine kinase as a therapeutic target in leukemia by Blanca Scheijen and James D. Griffin		93
6		JAK kinases in leukemias, lymphomas, and multiple myeloma by Renate Burger and Martin Gramatzki		115
7		Glivec (Gleevec, Imatinib, STI571) : a targeted therapy for chronic myelogenous leukemia by Elisabeth Buchdunger and Renaud Capedeville		145
8		Platelet-derived growth factor : normal function, role in disease, and application of PDGF antagonists by Tobias Sjoblom and Kristian Pietras and Arne Ostman and Carl-Henrik Heldin		161
9		Structural biology of protein tyrosine kinases by Sandra W. Cowan-Jacob and Paul Ramage and Wilhelm Stark and Gabriele Fendrich and Wolfgang Jahnke		187
10		Testing of signal transduction inhibitors in animal models of cancer by Terence O'Reilly and Robert Cozens		231
11		Phosphoproteomics in drug discovery and development by Michel F. Moran and Jarrod A. Marto and Cynthia J. Brame and Olga Ornatsky and Mark M. Ross and Leticia M. Toledo-Sherman and Alfredo C. Castro and Brett Larsen and Henry Duewel and Christopher Hosfield and Christopher Orsi and Thodoros Topaloglou and Daniel Figeys and Jennifer A. Caldwell-Busby and David R. Stover		265

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