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One pot desialylation and glycopegylation of therapeutic peptides

  • US 8,911,967 B2
  • Filed: 05/20/2010
  • Issued: 12/16/2014
  • Est. Priority Date: 08/19/2005
  • Status: Active Grant
First Claim
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1. A method of synthesizing a peptide conjugate comprising combining:

  • (a) sialidase;

    (b) an enzyme capable of catalyzing the transfer of a glycosyl linking group;

    (c) a modified sugar; and

    (d) a peptide,wherein the method comprises(i) a desialylation step in which the sialidase removes a sialic acid residue from the peptide, thereby forming a desialyated peptide, and(ii) a conjugation step in which the enzyme capable of catalyzing the transfer of a glycosyl linking group transfers a modified sugar moiety from the modified sugar to an amino acid or glycosyl residue of the peptide,which desialylation and conjugation steps are performed in the same vessel, thereby synthesizing the peptide conjugate.

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