[EN] PROCESS FOR THE MODIFICATION OF A GLYCOPROTEIN USING A ΒETA-(1,4)-N-ACETYLGALACTOSAMINYLTRANSFERASE OR A MUTANT THEREOF<br/>[FR] PROCÉDÉ POUR LA MODIFICATION D'UNE GLYCOPROTÉINE À L'AIDE D'UNE BÊTA-(1,4)-N-ACÉTYLGALACTOSAMINYL-TRANSFÉRASE OU D'UN MUTANT CORRESPONDANT
申请人:SYNAFFIX BV
公开号:WO2016022027A1
公开(公告)日:2016-02-11
The present invention relates to a process for the modification of a glycoprotein, using a β-(1,4)-N-acetylgalactosaminyltransferase or a mutant thereof.The process comprisesthe step of contacting a glycoprotein comprising a glycan comprising a terminal GlcNAc-moiety, in the presence of a β-(1,4)-N-acetylgalactosaminyl- transferase or a mutant thereof, with anon-natural sugar-derivative nucleotide.The non-natural sugar-derivative nucleotideis according to formula (3), wherein A is selected from the group consisting of -N3; -C(0)R3; -C=C-R4; -SH; -SC(0)R8; -SC(V)OR8, wherein V is O or S; -X wherein X is selected from the group consisting of F, CI, Br and I; -OS(0)2R5; an optionally substituted C2 - C24 alkyl group; an optionally substituted terminal C2 - C24 alkenyl group; and an optionally substituted terminal C3 - C24 allenyl group.
本发明涉及一种修饰糖蛋白的过程,使用β-(1,4)-N-乙酰半乳糖氨基转移酶或其突变体。该过程包括以下步骤:在β-(1,4)-N-乙酰半乳糖氨基转移酶或其突变体存在下,将含有末端GlcNAc基团的糖蛋白与一种非天然糖衍生核苷酸接触。该非天然糖衍生核苷酸符合以下公式(3),其中A选自-N3;-C(0)R3;-C=C-R4;-SH;-SC(0)R8;-SC(V)OR8,其中V为O或S;-X,其中X选自F、CI、Br和I;-OS(0)2R5;一个可选择取代的C2-C24烷基团;一个可选择取代的末端C2-C24烯基团;和一个可选择取代的末端C3-C24烯丙基团。