Polymer-Protein Conjugates - 1st Edition - ISBN: 9780444640819

Polymer-Protein Conjugates

1st Edition

From Pegylation And Beyond

Editors: Gianfranco Pasut Samuel Zalipsky
Paperback ISBN: 9780444640819
Imprint: Elsevier
Published Date: 1st November 2019
Page Count: 312
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Polymer–Protein Conjugates: From Pegylation and Beyond helps researchers by offering a unique reference and guide into this fascinating area. Sections cover the challenges surrounding the homogeneity of conjugates, their purity and polymer toxicity on long-term use, and how to deal with the risk of immunogenicity. These discussions help researchers design new projects by taking into account the latest innovations for safe and site selective polymer conjugation to proteins. PEG has been the gold standard and likely will play this role for many years, but alternatives are coming into the market, some of which have already been launched.

After five decades of improvements, the ideas in this book are entering into a new era of innovation because of the advances in genetic engineering, biochemistry and a better understanding of the results from clinical use of PEG conjugates in humans.

Key Features

  • Provides an overview on the state-of-the-art of protein polymer conjugation
  • Presents both the pros and cons of polymer-protein conjugates from the point-of-view of their clinical outcomes
  • Outlines advantages and potential risks of present technology based on PEG
  • Offers new alternatives for PEG and new approaches for on site-selective protein modification
  • Identifies future direction of research in this field


Graduate students and advanced researchers from academic/industrial background who are interested in protein modification and delivery. The potential users can be a pharmacologist, who want insight on this technology regarding approved product, as well as a biochemical engineer who wants learn how to design the future protein conjugates. Probably a chemist would be less involved although chemistry is at the basis of most successful conjugates. Patent attorney, PEGylation is described in many patents

Table of Contents

  1. Evolution of polymer conjugation to proteins
    Gianfranco Pasut and Samuel Zalipsky
    2. In vivo properties of therapeutic bioconjugates composed of proteins and architecturally/functionally complex polymers
    Ahlem Zaghmi, Andrea A Greschner, and Marc A Gauthier
    3. Protein modification by bis-alkylation
    Christina Picken, Sahar Awwad, Mire Zloh, Hanieh Khalili1 and Steve Brocchini
    4. Site-specific Polymer-protein conjugates by Cys mutation
    Nandini V. Katre
    5. Glycan-targeted PEGylation for selective modification of proteins
    M. Eugenia Giorgi, Rosalía Agusti and Rosa M. de Lederkremer
    6. Site-specific PEGylation of interferon beta-1b: from bench to clinic
    Natalie Winblade Nairn, Kenneth Grabstein,, Kurt D. Shanebeck, Gary Li, and Aijun Wang
    7. Enzymatic approaches to new protein conjugates
    Antonella Grigoletto, Katia Maso, Gianfranco Pasut
    8. Poly(2-oxazoline)-protein conjugates
    Ondrej Sedlacek, Victor R. de la Rosa, Richard Hoogenboom
    9. PEGylated Proteins: A Rational Design for Mitigating Clearance Mechanisms and Altering Biodistribution
    Maria J. Vicent and Mary Bossard
    10. PEGylation of human coagulation factor VIII and other plasma proteins
    Peter L. Turecek and Juergen Siekmann
    11. Immunogenicity assessment of PEGylated proteins, Lonquex, a PEGylated G-CSF case study
    Steffen Nock and Linglong Zou
    12. Pegvorhyaluronidase Alfa: A PEGylated Recombinant Human Hyaluronidase PH20 for the Treatment of Cancers That Accumulate Hyaluronan
    Daniel C. Maneval et al
    13. Challenges in the analytical characterization of PEGylated asparaginases
    Gunda Brandenburg et al
    14. Overcoming barriers for tumor-targeted drug delivery: the power of macromolecular anticancer drugs with the EPR effect and the modulation of vascular physiology
    Hiroshi Maeda and Waliul Islam
    15. Immunological responses to PEGylated proteins: anti-PEG antibodies
    Nehal E. Elsadek, Amr S. Abu Lila, Tatsuhiro Ishida
    16. PEG-protein conjugates: Non-clinical and clinical toxicity considerations
    Peter L. Turecek and Juergen Siekmann
    17. Polysialylation of human coagulation factor VIII
    Peter L. Turecek and Juergen Siekmann
    18. Polysaccharides for protein conjugation
    Elaine Ferguson et al
    19. PEG-Protein conjugates: regulatory requirements for characterization
    Mary J. Bossard
    20. Sialyltransferase mediated glycoPEGylation
    Carsten Behrens and Jens Buchardt


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© Elsevier 2020
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About the Editor

Gianfranco Pasut

Gianfranco Pasut, PhD is Full Professor of Pharmaceutical Technology at the University of Padua and has more than 20 years of research experience in the field of drug and protein delivery, in particular by polymer conjugation. He is an author of more than 70 peer-reviewed publications and 14 book chapters on polymer conjugation and an inventor of 9 patents. His research lab investigates new approaches of polymer conjugation, ADC and targeted liposome preparations and pioneered and expanded the use of the enzyme transglutaminase for the development of new conjugates.

Affiliations and Expertise

Head of Pasut’s Protein and Drug Delivery Lab, Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padova, Italy

Samuel Zalipsky

Samuel Zalipsky, Ph.D. is currently an independent consultant in the areas of carrier mediated drug delivery, nanoparticles, biocompatible polymers, liposomes, preparation and applications of a wide spectrum of bioconjugates, and PEGylated biopharmaceuticals in particular. His professional tenure of over 30 years was spent mainly in pharmaceutical industry, contributing to several commercialized technologies and products. He is an author of over 90 publications and listed as an inventor on over 50 patents.

Affiliations and Expertise

Independent Pharmaceutical Drug Delivery and Biotechnology Consultant

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