Inhibitors of binding between proteins and macromolecular ligands

摘要

Disclosed is a compound which inhibits binding between a target protein and a macromolecular ligand of the target protein. The compound comprises a targeting group, an attaching group and, optionally a linker group. In one aspect of the invention, the targeting group is a moiety that binds non-covalently to a surface of the target protein with a Kd of greater than about 0.1 μM and within sufficient proximity to the target protein/macromolecular ligand binding site to inhibit binding between the target protein and the macromolecular ligand. In another aspect of the invention, targeting group is degradable in vivo. In yet another aspect of the invention, the compound comprises a linker group that is cleavable in vivo.