A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics PDF
Preview A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics
Pier Andrea Borea Editor A Adenosine 3 Receptors from Cell Biology to Pharmacology and Therapeutics AB 3 A Adenosine Receptors from Cell Biology 3 to Pharmacology and Therapeutics Pier Andrea Borea Editor A Adenosine Receptors 3 from Cell Biology to Pharmacology and Therapeutics Editor Pier Andrea Borea Universita di Ferrara Sezione di Farmacologia Ferrara Italy ISBN 978-90-481-3143-3 e-ISBN 978-90-481-3144-0 DOI 10.1007/978-90-481-3144-0 Springer Dordrecht Heidelberg London New York Library of Congress Control Number: 2009930635 © Springer Science+Business Media B.V. 2010 No part of this work may be reproduced, stored in a retrieval system, or transmitted in any form or by any means, electronic, mechanical, photocopying, microfilming, recording or otherwise, without written permission from the Publisher, with the exception of any material supplied specifically for the purpose of being entered and executed on a computer system, for exclusive use by the purchaser of the work. Cover illustration: “MECA” (5¢-N-methylcarboxamidoadenosine) docked to the human A receptor. 3 Cover image was kindly provided by Dr. Andrei Ivanov, National Institutes of Health, Bethesda, MD Printed on acid-free paper Springer is part of Springer Science+Business Media (www.springer.com) Preface This book, with its 16 chapters, documents the present state of knowledge of the adenosine A receptor. It covers a wide range of information, including data from 3 studies of theoretical, molecular and cellular pharmacology, signal transduction, integrative physiology, new drug discoveries and clinical applications. It fills an important gap in the literature since no alternative source of such information is currently available. Although the A receptor is increasingly being recognized for 3 its increasing number of biological roles throughout the body and many A receptor 3 ligands have proven useful in elucidating peripheral and central pathologies, many issues remain unresolved. Moreover, research activity in this field continues to grow exponentially, resulting in a constant flow of new information. The chapters in this book cover both basic science and the relevant applications and provide an authoritative account of the current status of the field. They have enabled my goal as editor to make “A Adenosine Receptors from Cell Biology to Pharmacology and 3 Therapeutics” an up to date, scientifically excellent, reference source, attractive to basic and clinical scientists alike, a reality. Detailed understanding of the physico-chemical aspects and molecular biology of the A receptor provides a solid basis for its future development as a target for 3 adenosine-based pharmacotherapies (Chapters 2 and 3). Recognition and charac- terization of intracellular pathways modulated by A receptor activation supports 3 the belief that modulating these signaling routes is likely to lead to considerable advances in the management of many diseases (Chapters 4 and 5). The identifica- tion of new potent and selective A receptor ligands opens new frontiers for the 3 elucidation of the therapeutic potential arising from stimulating or blocking the A 3 receptor (Chapters 1, 6, 7 and 8). The A receptor appears to play a prominent role 3 under ischemic conditions and remains a promising target for promoting angio- genesis and treating neurodegenerative diseases associated with acute ischemia (Chapter 9). In terms of clinical utility, it will be critical to explore in greater detail the efficacy of the A receptor-mediated protective response in diseased hearts, 3 particularly with respect to diabetes, hypertension, hypertrophy, and dyslipidemias (Chapters 10 and 14). The important protective role of the adenosine A receptor, 3 originally discovered in studies of ischemia-reperfusion injury in the heart, has now been extended to skeletal muscle (Chapter 13). The importance of eosino- phils in allergy and asthma is well recognized and targeting the A receptor for the 3 v vi Preface treatment of eosinophil-dependent pulmonary diseases such as asthma, chronic obstructive pulmonary disease and rhinitis offers realistic hope of novel therapies (Chapters 1 and 11). A receptors are present in many immune cells and are 3 involved in the regulation of inflammatory and immune processes, suggesting new therapeutic strategies may emerge for inflammatory conditions such as sepsis, asthma and autoimmune disorders including rheumatoid arthritis, Crohn’s disease and psoriasis (Chapter 12). The oral bioavailability of certain A agonists and 3 encouraging data from early clinical studies support the development of these agents as anti-rheumatic drugs (Chapter 15). The effectiveness of the A receptor 3 agonist, Cl-IB-MECA, in several animal tumor models led to the introduction of this molecule into a program of pre-clinical and clinical studies. The excellent safety profile led to the initiation of clinical studies in patients with hepatocellular carcinoma which are currently ongoing. Paradoxically, it appears that A receptor 3 antagonists can also be considered promising in the treatment of human cancer (Chapter 16). These exciting results arising from the hard work of the people associated with this book hold promise for a future generation of new drugs for the treatment of important diseases. I would like to express my gratitude to the distinguished contributors who have expressed their confidence in this book by contributing to it and who will be key players in the success of the research on A receptors in the future. 2011–2012 will 3 mark the 20th anniversary of the cloning of the A receptor. It would give me enor- 3 mous pleasure if new molecules targeting the A receptor could become drugs at 3 this time with the help and participation of the eminent scientists who have authored this book. I would also like to thank very sincerely the Publishing Editor of Springer Biomedicine, Dr. Max Haring. It has been a pleasure working with him in this project. I am also extremely grateful for the critical contributions by Dr. John Fozard who has played a key role in the entire project. Last, but certainly not least, I wish to thank the members of my Research Group for their scientific work in the field of A adenosine receptors. 3 The first edition of “A Adenosine Receptors from Cell Biology to Pharmacology 3 and Therapeutics” volume is dedicated to my wife Cristina and to all the friends and colleagues who contributed to this book. Ferrara, Italy Prof. Pier Andrea Borea Contents Part I Introduction 1 From Hypertension (+) to Asthma: Interactions with the Adenosine A Receptor from a Personal Perspective .............. 3 3 John R. Fozard Part II Physico-chemical Properties and Molecular Biology 2 Thermodynamic Analysis in Drug–Receptor Binding: The A Adenosine Receptor ..................................................................... 29 3 Pier Andrea Borea, Stefania Gessi, Stefania Merighi, and Katia Varani 3 Pharmacology and Molecular Biology of A 3 Adenosine Receptors ................................................................................. 49 Karl-Norbert Klotz Part III Signal Transduction 4 Regulation of Second Messenger Systems and Intracellular Pathways ...................................................................... 61 Stefania Merighi, Carolina Simioni, Rob Lane, and Adriaan P. Ijzerman 5 The Desensitisation as A Adenosine Receptor Regulation: 3 Physiopathological Implications .............................................................. 75 Maria Letizia Trincavelli, Osele Ciampi, and Claudia Martini vii viii Contents Part IV Medicinal Chemistry 6 A Adenosine Receptor Agonists: History 3 and Future Perspectives ......................................................................... 93 Kenneth A. Jacobson, Zhan-Guo Gao, Dilip K. Tosh, Gangadhar J. Sanjayan, and Sonia de Castro 7 A Adenosine Receptor Antagonists: History and Future 3 Perspectives .............................................................................................. 121 Pier Giovanni Baraldi, Romeo Romagnoli, Giulia Saponaro, Stefania Baraldi, Mojgan Aghazadeh Tabrizi, and Delia Preti 8 Molecular Modeling and Reengineering of A 3 Adenosine Receptors ............................................................................... 149 Stefano Moro, Erika Morizzo, and Kenneth A. Jacobson Part V Effects on Tissues and Organs and Therapeutic Applications 9 Adenosine A Receptor Signaling in the Central 3 Nervous System ....................................................................................... 165 Felicita Pedata, Anna Maria Pugliese, Ana M. Sebastião, and Joaquim A. Ribeiro 10 Cardiovascular Biology of the A Adenosine Receptor ....................... 189 3 John P. Headrick, Jason N. Peart, Tina C. Wan, Wai-Meng Kwok, and John A. Auchampach 11 A Adenosine Receptor in the Pulmonary System ............................... 209 3 Yifat Klein and Idit Matot 12 A Adenosine Receptor Regulation of Cells of the Immune 3 System and Modulation of Inflammation ............................................. 235 Stefania Gessi, Valerio Sacchetto, Eleonora Fogli, and John Fozard 13 Adenosine A Receptors in Muscle Protection ..................................... 257 3 Bruce T. Liang, Maria Urso, Edward Zambraski, and Kenneth A. Jacobson 14 A Adenosine Receptors, HIF-1 Modulation 3 and Atherosclerosis ................................................................................. 281 Stefania Gessi, Stephen MacLennan, Edward Leung, and Pier Andrea Borea Contents ix Part VI Inflammatory and Auto-Immune Diseases 15 Rheumatoid Arthritis: History, Molecular Mechanisms and Therapeutic Applications ................................................................ 291 Pnina Fishman and Sara Bar-Yehuda Part VII Cancer 16 Agonists and Antagonists: Molecular Mechanisms and Therapeutic Applications ................................................................ 301 Pnina Fishman, Sara Bar-Yehuda, Katia Varani, Stefania Gessi, Stefania Merighi, and Pier Andrea Borea Index ................................................................................................................. 319 Contributors John A. Auchampach Department of Pharmacology, Medical College of Wisconsin, Milwaukee, WI 53226 [email protected] Pier Giovanni Baraldi Department of Pharmaceutical Sciences, University of Ferrara, Via Fossato di Mortara 17/19b, 44100 Ferrara, Italy [email protected] Stefania Baraldi Department of Pharmaceutical Sciences, University of Ferrara, Via Fossato di Mortara 17/19b, 44100 Ferrara, Italy [email protected] Sara Bar-Yehuda Can-Fite BioPharma, 10 Bareket st., Kiryat Matalon, Petach-Tikva, 49170, Israel, [email protected] Pier Andrea Borea Department of Clinical and Experimental Medicine, Pharmacology Unit, University of Ferrara, via Fossato di Mortara 17-19, 44100 Ferrara, Italy [email protected] Osele Ciampi Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno, 6, 56126 Pisa, Italy [email protected] Sonia de Castro Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA [email protected] xi
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