abstract |
The present invention relates to a process for the enzymatic modification of a glycoprotein. The process comprises the step of contacting a glycoprotein comprising a glycan comprising a terminal GlcNAc-moiety, in the presence of glycosyltransferase that is, or is derived from, a β-(1,4)-N-acetylgalactosaminyltransferase, with a non-natural sugar-derivative nucleotide. The non-natural sugar-derivative nucleotide is according to formula (3): n n n n n n n n n n wherein A is selected from the group consisting of —N 3 , —C(O)R 3 , —(CH 2 ) i C≡C—R 4 , —SH, —SC(O)R 8 , —SC(O)OR 8 , —SC(S)OR 8 , —F, —Cl, —Br —I, —OS(O) 2 R 5 , terminal C 2 -C 24 alkenyl groups, C 3 -C 5 cycloalkenyl groups, C 4 -C 8 alkadienyl groups, terminal C 3 -C 24 allenyl groups and amino groups. The invention further relates to a glycoprotein obtainable by the process according to the invention, to a bioconjugate that can be obtained by conjugating the glycoprotein with a linker-conjugate, and to β-(1,4)-N-acetylgalactosaminyltransferases that can be used in preparing the glycoprotein according to the invention. |