E-Book Overview
This volume focuses on screening and profiling kinase inhibitors or activators. Chapters in this book cover several facets of the drug discovery processes starting with target identification, and assay development and screening chemical libraries for hit identification and lead optimization. The profiling portion of Kinase Screening and Profiling: Methods and Protocols discusses several strategies and techniques that are required to minimize off target hits and reduce cellular toxicities that are caused by liability kinases. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls.
Timely and authoritative, Kinase Screening and Profiling: Methods and Protocols, will benefit scientists and researchers who are interested in exploring the role of kinases in academic, as well as pharmaceutical research.
E-Book Content
Methods in Molecular Biology 1360
Hicham Zegzouti Said A. Goueli Editors
Kinase Screening and Profiling Methods and Protocols
METHODS
IN
MOLECULAR BIOLOGY
Series Editor John M. Walker School of Life and Medical Sciences University of Hertfordshire Hatfield, Hertfordshire, AL10 9AB, UK
For further volumes: http://www.springer.com/series/7651
Kinase Screening and Profiling Methods and Protocols
Edited by
Hicham Zegzouti and Said A. Goueli Promega Corporation, Madison, Wisconsin, USA
Editors Hicham Zegzouti Promega Corporation Madison, WI, USA
Said A. Goueli Promega Corporation Madison, WI, USA
ISSN 1064-3745 ISSN 1940-6029 (electronic) Methods in Molecular Biology ISBN 978-1-4939-3072-2 ISBN 978-1-4939-3073-9 (eBook) DOI 10.1007/978-1-4939-3073-9 Library of Congress Control Number: 2015951783 Springer New York Heidelberg Dordrecht London © Springer Science+Business Media New York 2016 This work is subject to copyright. All rights are reserved by the Publisher, whether the whole or part of the material is concerned, specifically the rights of translation, reprinting, reuse of illustrations, recitation, broadcasting, reproduction on microfilms or in any other physical way, and transmission or information storage and retrieval, electronic adaptation, computer software, or by similar or dissimilar methodology now known or hereafter developed. The use of general descriptive names, registered names, trademarks, service marks, etc. in this publication does not imply, even in the absence of a specific statement, that such names are exempt from the relevant protective laws and regulations and therefore free for general use. The publisher, the authors and the editors are safe to assume that the advice and information in this book are believed to be true and accurate at the date of publication. Neither the publisher nor the authors or the editors give a warranty, express or implied, with respect to the material contained herein or for any errors or omissions that may have been made. Printed on acid-free paper Humana Press is a brand of Springer Springer Science+Business Media LLC New York is part of Springer Science+Business Media (www.springer.com)
Preface Protein kinases play a central role in cellular physiology and diverse biological processes and thus alterations in their expression or activity have considerable consequences. Based on the critical role they play in regulation of normal and abnormal cellular growth and differentiation, these enzymes prove to be very valuable therapeutic targets. It has been estimated that over 60% of current discovery programs in pharmaceutical companies are focused on protein kinase inhibitors. As of 201