| CPC A61K 47/6807 (2017.08) [A61K 31/713 (2013.01); A61K 47/60 (2017.08); A61K 47/64 (2017.08); A61K 47/6811 (2017.08); A61K 47/6849 (2017.08); A61K 47/6883 (2017.08); A61P 35/00 (2018.01); C07H 17/00 (2013.01); C07K 16/2863 (2013.01); C12N 15/113 (2013.01); C12N 2310/312 (2013.01); C12N 2310/3125 (2013.01); C12N 2310/315 (2013.01); C12N 2310/3513 (2013.01); C12N 2310/3515 (2013.01)] | 12 Claims |
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1. A polynucleotide conjugate molecule comprising a binding moiety, a polynucleotide, a linker selected from succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC), N-succinimidyl 3-(2-pyridyldithio)propionate (SPDP) or bis-maleimide (BisMal);
wherein the polynucleotide comprises at least one 5′-vinylphosphonate modified non-natural nucleotide, and at least one modified internucleotide linkage or at least one inverted abasic moiety; and wherein the at least one 5′-vinylphosphonate modified non-natural nucleotide is
![]() wherein B is a heterocyclic base moiety;
wherein the polynucleotide comprises a double-stranded polynucleic acid molecule comprising a guide strand and a passenger strand, wherein the at least one 5′-vinylphosphonate modified non-natural nucleotide is located at 5′-terminus of the guide strand and the binding moiety is conjugated to 5′-terminus of the passenger strand; and
wherein the binding moiety is an antibody or antigen binding fragment thereof that recognizes a cell surface protein.
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