Polymer-Protein Conjugates

Polymer-Protein Conjugates

From Pegylation and Beyond

1st Edition - October 30, 2019

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  • Editors: Gianfranco Pasut, Samuel Zalipsky
  • Paperback ISBN: 9780444640819
  • eBook ISBN: 9780444640826

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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 backgrounds who are interested in protein modification and delivery. The potential users can be pharmacologists, who want insight on this technology regarding approved product, as well as a biochemical engineers, who wants to learn how to design future protein conjugates. Probably a chemist would be less involved although chemistry is at the basis of most successful conjugates. Patent attorneys, since PEGylation is described in many patents

Table of Contents

  • Introduction and General Aspects of the Technology
    1. Evolution of Polymer Conjugation to proteins
    Samuel Zalipsky and Gianfranco Pasut
    2. PEGylated Proteins: A Rational Design for Mitigating Clearance Mechanisms and Altering Biodistribution
    Maria J. Vicent and Mary Bossard
    3. 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

    Toxicity and Immunogenicity Studies and Clinical Stage Conjugate Products
    4. PEG-protein conjugates: Non-clinical and clinical toxicity considerations
    Peter L. Turecek and Juergen Siekmann
    5. Immunological responses to PEGylated proteins: anti-PEG antibodies
    Nehal E. Elsadek, Amr S. Abu Lila, and Tatsuhiro Ishida
    6. Immunogenicity assessment of PEGylated proteins, Lonquex, a PEGylated G-CSF case study
    Steffen Nock and Linglong Zou
    7. PEG-Protein conjugates: regulatory requirements for characterization
    Mary J. Bossard
    8. PEGylation of human coagulation factor VIII and other plasma proteins
    Peter L. Turecek and Juergen Siekmann
    9. Pegvorhyaluronidase Alfa: A PEGylated Recombinant Human Hyaluronidase PH20 for the Treatment of Cancers That Accumulate Hyaluronan
    Daniel C. Maneval, Chris Caster, Celine Derunes, et al.
    10. Challenges in the analytical characterization of PEGylated asparaginases
    Gunda Brandenburg, Sabine Poppenborg, Christoph Radcke, et al.

    Novel Site-Selective Methods of Conjugation
    11. Glycan-targeted PEGylation for selective modification of proteins
    M. Eugenia Giorgi, Rosalía Agusti and Rosa M. Lederkremer
    12. Sialyltransferase mediated glycoPEGylation
    Carsten Behrens and Jens Buchardt
    13. Enzymatic approaches to new protein conjugates
    Antonella Grigoletto, Katia Maso, and Gianfranco Pasut
    14. Site-specific Polymer-protein conjugates by Cys mutation
    Nandini V. Katre
    15. Site-specific PEGylation of interferon beta-1b: from bench to clinic
    Natalie Winblade Nairn
    16. Protein modification by bis-alkylation
    Christina Picken, Sahar Awwad, Mire Zloh, Hanieh Khalili, and Steve Brocchini

    Alternative non-PEG polymers and architectures
    17. In vivo properties of therapeutic bioconjugates composed of proteins and architecturally/functionally complex polymers
    Ahlem Zaghmi, Andrea A Greschner, and Marc A. Gauthier
    18. Poly(2-oxazoline)-protein conjugates
    Ondrej Sedlacek, Victor R. de la Rosa, and Richard Hoogenboom
    19. Polysaccharides for protein and peptide conjugation
    Elaine L. Ferguson, Mathieu Varache, Joana Stokniene and David W. Thomas
    20. Polysialylation of human coagulation factor VIII
    Peter L. Turecek and Juergen Siekmann

Product details

  • No. of pages: 512
  • Language: English
  • Copyright: © Elsevier 2019
  • Published: October 30, 2019
  • Imprint: Elsevier
  • Paperback ISBN: 9780444640819
  • eBook ISBN: 9780444640826

About the Editors

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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