Compositions and methods for the synthesis and identification of covalent aptamers
AssigneeUniversity of Hawaii
InventorIain Seido MacPHERSON
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Abstract
Compositions and methods for preparing and identifying aptamers and aptamer-protein conjugates are provided. The use of a nucleotide analog functionalized with an amine-reactive cross-linker facilitates covalent cross-linking of the aptamer to a protein, in particular site-specific cross-linking to the Fc domain of an antibody.
Claims19
An aptamer library for identifying a target protein capable of covalent binding to at least one aptamer of said library comprising a plurality of aptamers each having at least one nucleotide analog functionalized with an amine-reactive cross-linker.
An Fc-aptamer conjugate comprising
- (a) an Fc polypeptide;
- and
- (b) an aptamer that specifically binds to a first site on the Fc polypeptide, the aptamer comprising at least one nucleotide analog functionalized with an amine-reactive cross-linker,
- wherein the Fc polypeptide and aptamer are conjugated via the amine-reactive cross-linker of the aptamer and a primary amine at a second site on the Fc polypeptide proximal to the first site on the Fc polypeptide.
An aptamer that specifically binds to an Fc region of:
- (a) mouse IgG1 or IgG2, the aptamer comprising the nucleotide sequence AGCGCGGAACCGXGCCXGGC (SEQ ID NO:1) or XAACGCARXAAGCGAG (SEQ ID NO:2), or
- (b) human IgG1, the aptamer comprising the nucleotide sequence CAAXGGCAACAXGCACACAGA (SEQ ID NO:3),
- wherein at least one X is a nucleotide analog.
A phosphoramidite comprising the structure of Formula I:
- wherein R1 is H, O-methyl, dimethyl, fluoro, amino, C-allyl, arabinofluoro, methylene, difluoromethylene or a protecting group;
- and R2 is a protecting group.
Dependencies are inferred from the claim text.