Discovery of a new inhibitor targeting PD-L1 for cancer immunotherapy.

ABSTRACT: Blockade of the PD-1/PD-L1 immunologic checkpoint using monoclonal antibodies has provided breakthrough therapies against cancer in the recent years. Nevertheless, intrinsic disadvantages of therapeutic antibodies may limit their applications. Thus, blocking of the PD-1/PD-L1 interaction by small molecules may be a promising alternative for cancer immunotherapy. We used a docking-based virtual screening strategy to rapidly identify new small molecular inhibitors targeting PD-L1. We demonstrated that a small molecule compound (N-[2-(aminocarbonyl)phenyl][1,1'-biphenyl]-4-carboxamide [APBC]) could effectively interrupt the PD-1/PD-L1 interaction by directly binding to PD-L1, presenting the K_D and IC₅₀ values at low-micromolar level. Molecular docking study revealed that

SUBMITTER: Wang F 

PROVIDER: S-EPMC7851350 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature