Targeting compounds
AssigneeThe Scripps Research Institute
InventorsCarlos F. Barbas, Christoph Rader, Subhash C. Sinha, Richard A. Lerner
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Abstract
The present invention provides antibody targeting compounds in which the specificity of the antibody has been reprogrammed by covalently or noncovalently linking a targeting agent to the combining site of an antibody. By this approach, the covalently modified antibody takes on the binding specificity of the targeting agent. The compound may have biological activity provided by the targeting agent or by a separate biological agent. Various uses of the invention compounds are provided.
Claims21
A targeting compound comprising an antibody or an antigen binding fragment thereof and a therapeutic targeting agent at least 300 Daltons in size linked to a side chain of a reactive lysine residue in the combining site of the antibody or antigen binding fragment thereof via a linker comprising X, wherein a precursor of the linker comprises the formula X—Z, wherein X is a linear or branched connecting chain of atoms comprising any of C, H, N, O, P, S, Si, F, Cl, Br, and I, or a salt thereof, and wherein Z is a group that competes for reaction with the side chain of the reactive lysine residue in the combining site of the antibody or antigen binding fragment thereof with a reactive group having the structure:
- wherein the therapeutic targeting agent is linked via X to the side chain of the reactive lysine residue in the combining site of the antibody or antigen binding fragment thereof by an amine or amide linkage formed by contacting Z and the side chain of the reactive lysine residue in the combining site of the antibody or antigen binding fragment thereof.
Dependencies are inferred from the claim text.