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US 2024/0053333 A1Published application
Chemical modification of antibodies and functional fragments thereof
AssigneeNautilus Subsidiary, Inc.
InventorsSeok Ki CHOI, Julia ROBINSON
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Abstract
Provided are antibody conjugates, including a pair of cysteines crosslinked via a two-carbon bridge covalently connecting the sulfur atoms of the cysteines. Methods for making and using antibody conjugates are also provided. The compositions and methods of the present disclosure although particularly well suited to antibodies can be extended to other analytes having sulfur moieties such as proteins obtained from biological or artificial sources.
Claims20
A method of modifying an antibody comprising
- reacting cysteines of an antibody with an alkyne moiety of a modifying reagent, wherein the alkyne moiety reacts with the cysteines to form a moiety of Formula I:
- wherein S comprises the sulfur moieties of the cysteines, and
- wherein R1, R2, R3, and R4 are each independently selected from the group consisting of hydrogen, halo, alkyl, alkenyl, alkynyl, aryl, heteroalkyl, heteroalkenyl, heteroalkynyl, heteroaryl, and optionally substituted variants thereof.
An antibody, comprising a pair of cysteines crosslinked via a moiety of Formula I:
- wherein S comprises the sulfur moieties of the cysteines, and
- wherein R1, R2, R3, and R4 are each independently selected from the group consisting of hydrogen, halo, alkyl, alkenyl, alkynyl, aryl, heteroalkyl, heteroalkenyl, heteroalkynyl, heteroaryl, and optionally substituted variants thereof.
Dependencies are inferred from the claim text.