| 主权项 |
1. A glycoprotein-toxic payload molecule conjugate represented by formula I
[D-L-G]n-Gp Formula I wherein Gp is a glycoprotein comprising an N-glycan, wherein the N-glycan comprises a GlcNAc residue bound by a β-N linkage to an asparagine; n is an integer from 1 to about 20; D is a toxic payload molecule; L is a linker group covalently joining G to D; and G is a saccharide structure represented by formula II wherein R is a glycosidic bond to the N-glycan or a glycosidic bond to the GlcNAc residue bound by a β-N linkage to an asparagine; X1 is H or carboxyl; X2, X3 and X4 are each independently OH, H, amino, C2-C6 acylamide, phosphate or sulphate ester, or a bond to L; X5 is CH2OH, carboxyl, CH3, H, C1-C3 alkyl or substituted C1-C3 alkyl, or a bond to L; with the proviso that one substituent selected from X2, X3, X4 and X5 is a bond to L or bonded via a bond to L; and with the proviso that when X1 is carboxyl, then X2 is H, X3 is OH, X5 is C1-C3 alkyl or substituted C1-C3 alkyl; R is a glycosidic bond to the N-glycan; and X4 is a bond to L or X5 is bonded via a bond to L; or when X1 is H, then R is a glycosidic bond to the N-glycan or to the GlcNAc residue bound by a β-N linkage to an asparagine. |
