公开(公告)号：US20210315856A1

公开(公告)日：2021-10-14

申请号：US17356751

申请日：2021-06-24

Applicant: Arvinas Operations, Inc.

Inventor： Andrew P. Crew ,  Hanging Dong ,  Brain Hamman ,  Taavi K. Neklesa ,  Yimin Qian ,  Jing Wang ,  Kurt Zimmermann

IPC: A61K31/277 ,  G16B20/00 ,  A61K47/55 ,  G16C20/50 ,  G16B15/30 ,  G16B20/30 ,  A61K31/4166 ,  A61K31/551 ,  A61K38/05 ,  G01N33/68

Abstract: The present disclosure is based on the surprising and unexpected discovery that a ligand molecule with certain characteristics is able to bind to two protein molecules simultaneously and recruit them to form a transient or stable protein-protein interaction complex. The protein-protein interaction and other cross-domain interactions gained in this process contribute additional stabilization energy to the complex beyond the combination of the binary binding energies, and therefore, largely increase the binding potency of the ligand. Accordingly, the present disclosure provides a Protein-Protein Interaction Inducing Technology (PPIIT), which includes a method to design and identify the tripartite or bifunctional compounds and use such compounds to induce protein-protein interactions in various contexts. The present disclosure also provides a composition for the purpose of inducing protein-protein interactions.