PEGylated Protein Drugs: Basic Science and Clinical Applications

PEGylated Protein Drugs: Basic Science and Clinical Applications describes the basic technologies and the major results obtained with the PEGylation technique, the covalent binding to proteins, peptides and small organic molecules of the hydrophilic and b

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Milestones in Drug Therapy MDT

Series Editors Prof. Dr. Michael J. Parnham PhD Director of Preclinical Discovery Centre of Excellence in Macrolide Drug Discovery GlaxoSmithKline Research Centre Zagreb Ltd. Prilaz baruna Filipovi´ca 29 HR-10000 Zagreb Croatia

Prof. Dr. J. Bruinvels Sweelincklaan 75 NL-3723 JC Bilthoven The Netherlands

PEGylated Protein Drugs: Basic Science and Clinical Applications Edited by Francesco M. Veronese

Birkhäuser Basel · Boston · Berlin

Editors Francesco M. Veronese Department of Pharmaceutical Sciences University of Padova 35131 Padova Italy

Advisory Board J.C. Buckingham (Imperial College School of Medicine, London, UK) R.J. Flower (The William Harvey Research Institute, London, UK) A.G. Herman (Universiteit Antwerpen, Antwerp, Belgium) P. Skolnick (NYU Langone Medical Center, New York, NY, USA)

Library of Congress Control Number: 2009928445

Bibliographic information published by Die Deutsche Bibliothek Die Deutsche Bibliothek lists this publication in the Deutsche Nationalbibliografie; detailed bibliographic data is available in the Internet at .

ISBN 978-3-7643-8678-8 Birkhäuser Verlag, Basel - Boston - Berlin The publisher and editor can give no guarantee for the information on drug dosage and administration contained in this publication. The respective user must check its accuracy by consulting other sources of reference in each individual case. The use of registered names, trademarks etc. in this publication, even if not identified as such, does not imply that they are exempt from the relevant protective laws and regulations or free for general use. This work is subject to copyright. All rights are reserved, whether the whole or part of the material is concerned, specifically the rights of translation, reprinting, re-use of illustrations, recitation, broadcasting, reproduction on microfilms or in other ways, and storage in data banks. For any kind of use, permission of the copyright owner must be obtained. © 2009 Birkhäuser Verlag, P.O. Box 133, CH-4010 Basel, Switzerland Part of Springer Sciebnce+Business Media Printed on acid-free paper produced from chlorine-free pulp. TCF ∞ Cover illustration: see p. 191. Reproduced with kind permission of Taylor and Francis Group LLC. Printed in Germany ISBN 978-3-7643-8678-8

987654321

e-ISBN: 978-3-7643-8679-5 www.birkhauser.ch

V

Contents List of contributors . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .

VII

Ruth Duncan and Francesco M. Veronese Preface: PEGylated protein conjugates: A new class of therapeutics for the 21st century . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .

1

Francesco M. Veronese, Anna Mero and Gianfranco Pasut Protein PEGylation, basic science and biological applications . . . . . . .

11

Gian Maria Bonora and Sara Drioli Reactive PEGs for protein conjugation . . . . . . . . . . . . . . . . . . . . . . . . .

33

Ji-Won Choi, Antony Godwin, Sibu Balan, Penny Bryant, Yuehua Cong, Estera Pawlisz, Manuchehr Porssa, Norbert Rumpf, Ruc