Akt-specific capture agents, compositions, and methods of using and making

摘要

The present application provides stable peptide-based Akt capture agents and the use thereof as detection, diagnosis, and treatment agents. The application further provides novel methods of developing stable peptide-based capture agents, including Akt capture agents, using iterative on-bead in situ click chemistry.

主权项

1. A stable, synthetic capture agent that specifically binds Akt, wherein the capture agent comprises an anchor ligand, a secondary ligand, and optionally a tertiary ligand,
wherein the capture agent binds to a non-ATP and non-peptide substrate binding site of Akt and wherein the capture agent is capable of allosterically inhibiting Akt activity upon binding to the binding site, wherein said anchor ligand comprises the peptide sequence Az8-VFYRLGY-CONH2 (SEQ ID NO: 17), wherein Az8 represents and azide amino acid having the structure: