G Protein-Coupled Receptor Kinases

This collection explores up-to-date descriptions of known G protein-coupled receptor kinase (GRK)-dependent mechanisms, both associated with G protein-coupled receptor (GPCR) functions and the receptor-independent. The chapters cover a wide range of studi

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Vsevolod V. Gurevich Eugenia V. Gurevich John J.G. Tesmer Editors

G ProteinCoupled Receptor Kinases

METHODS AND

IN

PHARMACOLOGY

TOXICOLOGY

Series Editor Y. James Kang University of Louisville School of Medicine Prospect, Kentucky, USA

For further volumes: http://www.springer.com/series/7653

G Protein-Coupled Receptor Kinases Edited by

Vsevolod V. Gurevich Department of Pharmacology, Vanderbilt University, Nashville, TN, USA

Eugenia V. Gurevich Department of Pharmacology, Vanderbilt University, Nashville, TN, USA

John J.G. Tesmer Life Sciences Institute, University of Michigan, Ann Arbor, MI, USA

Editors Vsevolod V. Gurevich Department of Pharmacology Vanderbilt University Nashville, TN, USA

Eugenia V. Gurevich Department of Pharmacology Vanderbilt University Nashville, TN, USA

John J.G. Tesmer Life Sciences Institute University of Michigan Ann Arbor, MI, USA

ISSN 1557-2153 ISSN 1940-6053 (electronic) Methods in Pharmacology and Toxicology ISBN 978-1-4939-3796-7 ISBN 978-1-4939-3798-1 (eBook) DOI 10.1007/978-1-4939-3798-1 Library of Congress Control Number: 2016942568 © 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 This Humana Press imprint is published by Springer Nature The registered company is Springer Science+Business Media LLC New York

Preface The signaling by most G protein-coupled receptors (GPCRs) is regulated by a conserved two-step mechanism: phosphorylation of active receptor by G protein-coupled receptor kinases (GRKs) followed by specific binding of an arrestin protein to the active phosphoreceptor. Arrestin binding blocks further coupling of the receptor to G proteins, promotes the recruitment of the complex to coated pits for internalization, and initiates a second, G protein-independent round of signaling. Whereas GPCRs, G proteins, and arrestins are getting a lot of attention, GRKs remain underestimated and under-investigated players in the regulation of GPCR signa