申请人:SYNAFFIX B.V.
公开号:US20160250347A1
公开(公告)日:2016-09-01
Glycoproteins comprising a glycan of the formula (102) are disclosed; wherein b is 0 or 1; the GlcNAc residue optionally fucosylated; and Su(A)
x
is a sugar derivative comprising x functional groups A, wherein x is 1, 2, 3 or 4 and A is independently selected from the group consisting of an azido group, a keto group, an alkynyl group, a thiol group, a halogen, a sulfonyloxy group, a halogenated acetamido group, a mercaptoacetamido group and a sulfonylated hydroxyacetamido group.
Protein-conjugates having glycoproteins according to the invention conjugated to a molecule of interest (e.g., an active substance) are also disclosed. Examples include modified antibodies, antibody-conjugates, and antibody-drug conjugates (ADCs). Processes for the preparation of the modified glycoproteins according to the invention and methods for the preparation of a protein-conjugate according to the invention are mentioned.
本发明揭示了一种包含公式(102)的糖蛋白;其中b为0或1;GlcNAc残基可以选择性地被岩藻糖基化;Su(A)是一种糖衍生物,包括x个功能基团A,其中x为1、2、3或4,A独立地选择自由基组,包括偶氮基、酮基、炔基、硫醇基、卤素、磺酰氧基、卤代乙酰胺基、巯基乙酰胺基和磺酰化羟基乙酰胺基。
本发明还揭示了将本发明中的糖蛋白共轭到感兴趣的分子(例如,活性物质)上的蛋白质共轭物。例如,包括改性抗体、抗体共轭物和抗体药物共轭物(ADC)。还提及了制备本发明中改性糖蛋白的方法以及制备本发明中蛋白质共轭物的方法。