Enzymatic techniques for PEGylation of biopharmaceuticals

  • Mauro Sergi
  • Francesca Caboi
  • Carlo Maullu
  • Gaetano Orsini
  • Giancarlo Tonon
Part of the Milestones in Drug Therapy book series (MDT)


Modification of therapeutic proteins and peptides by polyethylene glycol conjugation is a well known method to improve the pharmacological properties of such drugs.

Here we describe an alternative way of PEGylation from classic chemical methods, taking advantage of enzymes able to specifically modify some amino acid side chains, in particular glycosyltransferases and transglutaminases.

A few examples are here described, in particular granulocyte-colony stimulating factor, which has been successfully PEGylated by enzymatic methods leading to a new long-lasting compound presently under evaluation in clinical studies.


Acyl Acceptor Enzymatic Technique Microbial Transglutaminase Adenosine Deaminase Deficiency Protein PEGylation 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


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Copyright information

© Birkhäuser Verlag/Switzerland 2009

Authors and Affiliations

  • Mauro Sergi
    • 1
    • 2
  • Francesca Caboi
    • 1
  • Carlo Maullu
    • 1
  • Gaetano Orsini
    • 1
  • Giancarlo Tonon
    • 1
  1. 1.Bio-Ker S.r.lParco Scientifico e Tecnologico della SardegnaPula, CagliariItaly
  2. 2.Ablynx nvZwijnaardeBelgium

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