Genequantum Healthcare (suzhou) Co., Ltd.

Meijun Xiong

Gang Qin

Cao Lv

Jinduo Yuan

Mingyu Hu

A method for preparing an antibody-drug conjugate. The antibody-drug conjugate is formed by means of site-directed conjugation on the basis of an N-glycosylation site of an Fc region of an antibody. The method comprises: (1) providing a donor containing an oxazoline oligosaccharide, an antibody containing a GlcNAc motif, and an immobilized endoglycosidase having a glycoside transfer activity; and (2) covalently linking the activated donor containing the oxazoline oligosaccharide to the antibody containing the GlcNAc motif by means of the catalytic action of the endoglycosidase; therefore, one-step conjugation is realized. The present invention also relates to an endoglycosidase fusion protein, which comprises a covalently linked endoglycosidase, a Halo tag, and/or a His tag. The present invention also relates to an immobilized endoglycosidase fusion protein obtained by means of immobilizing an endoglycosidase fusion protein on a support, a prepacked column filled with the immobilized fusion protein, and a method for purifying an antibody conjugate by using the immobilized endoglycosidase fusion protein.

Immobilized endoglycosidase fusion protein and use thereof

The present disclosure further relates to a linker-payload compound including an oligosaccharide group, especially a disaccharide group, where the oligosaccharide group is linked to the remainder of the compound by an amide bond. The present disclosure further relates to an antibody-drug conjugate (ADC) containing the linker-payload compound, where the glycan chain in an antibody is remodeled with the oligosaccharide moiety in the linker-payload compound. The present disclosure further relates to preparation methods and use of the above-mentioned substances.

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Suzhou, China

Meijun Xiong