[EN] MODIFIED ANTIBODY, ANTIBODY-CONJUGATE AND PROCESS FOR THE PREPARATION THEREOF<br/>[FR] ANTICORPS MODIFIÉ, ANTICORPS-CONJUGUÉ ET PROCÉDÉ DE PRÉPARATION ASSOCIÉ
申请人:SYNAFFIX BV
公开号:WO2014065661A1
公开(公告)日:2014-05-01
The present invention relates to an antibody comprising a GlcNAc-S(A)x substituent, wherein S(A)x is a sugar derivative comprising x functional groups A wherein A is independently selected from the group consisting of an azido group, a keto group and an alkynyl group and x is 1, 2, 3 or 4, wherein said GlcNAc-S(A)x substituent is bonded to the antibody via CI of the N-acetylglucosamine of said GlcNAc-S(A)x substituent, and wherein said N-acetylglucosamine is optionally fucosylated. The invention also relates to an antibody-conjugate, in particular to an antibody- conjugate according to the Formula (20) or (20b), wherein AB is an antibody, S is a sugar or a sugar derivative, D is a molecule of interest, and wherein said N- acetylglucosamine is optionally fucosylated (b is 0 or 1). The invention further relates to a process for the preparation of a modified antibody, to a process for the preparation of an antibody-conjugate, and to said antibody-conjugate for use as a medicament. In addition, the invention relates to a kit of parts comprising an azide-modified antibody and a linker-conjugate, wherein said linker-conjugate comprises a (hetero)cycloalkynyl group and one or more molecules of interest.
本发明涉及一种包含GlcNAc-S(A)x取代基的抗体,其中S(A)x是一种包含x个功能基团A的糖衍生物,其中A是从包括偶氮基、酮基和炔基的组中独立选择的,x为1、2、3或4,其中所述的GlcNAc-S(A)x取代基通过所述的GlcNAc-S(A)x取代基的N-乙酰葡萄糖胺的CI与抗体结合,其中所述的N-乙酰葡萄糖胺可选择地被岩藻糖化。本发明还涉及一种抗体结合物,特别是根据式(20)或(20b)的抗体结合物,其中AB是一种抗体,S是一种糖或糖衍生物,D是一种感兴趣的分子,其中所述的N-乙酰葡萄糖胺可选择地被岩藻糖化(b为0或1)。本发明还涉及一种改性抗体的制备方法,一种抗体结合物的制备方法,以及用作药物的所述抗体结合物。此外,本发明还涉及一种部件套件,包括偶氮基修饰的抗体和连接物结合物,其中所述的连接物结合物包括(杂)环炔基团和一个或多个感兴趣的分子。