Novel PEGylation keeping high protein activity

Single Step Reaction, No Need of Genetic Modification

Advantages

  • Maintains original structures and functions with less basicity changes, mild reaction
  • Less variants, no bi-products helps easy purification, low cost production
  • Demonstrated more than 20x activity than conventionally-PEGylated lysozyme (fig-R)

Background and Technology

Modification with polyethylene glycol (PEGylation) is widely used for stabilizing biologic drugs (protein,
peptide, etc.). PEGylation with activated esters is conventionally used, but it deteriorates functionality
of molecules due to structural changes due to neutralization of amino group into amide, non-specific
additions, and harsh reaction conditions.
The newly developed bifurcated aldehyde group functionalized polyethylene glycol (PEG-GALD)
PEGylation technology improves the issues. PEG-GALD specifically reacts with primary amine of
peptides at neutral pH, room temperature, and forms the same basic tertial amine without bi-product
emission (fig-L).

Patent

Granted: JP(5999659), US (9327034)

Researcher

Prof. Y. Nagasaki and Assoc. prof. Y. Ikeda, Faculty of Pure & Appl Sci, Univ. of Tsukuba

Publication

Bioconjugate Chem. 2013, 24, 1824−1827(doi.org/10.1021/bc400169s)

Expectations

License for biologics development and reformulation. Evaluation pattern would be;
1) material transfer: sending PEG-GALD to companies for inhouse evaluation,
2) collaborative research: Univ’s lab. evaluates characteristics of proteins from companies.

Product No. MR-03995

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