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Updated: Aug 29, 2025

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
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Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries

Published on: January 22, 2019

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Development of Inhibitors Targeting the V-Domain Ig Suppressor of T Cell Activation Signal Pathway

Shuai Zheng1, Kuojun Zhang1, Xiangyu Zhang1

  • 1Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.

Journal of Medicinal Chemistry
|September 9, 2022
PubMed

Blockade of cytotoxic T lymphocyte antigen 4 (CTLA-4) and programmed cell death-1/programmed cell death-ligand 1 (PD-1/PD-L1) has produced considerable therapeutic effect, but only in a fraction of patients, so more targets are being investigated. VISTA (V-domain Ig suppressor of T cell activation) is a novel immune checkpoint that is broadly expressed within hematopoietic cells and multiple cancers (low expressing frequency on solid tumors), particularly those with a poor immunotherapy response rate. As a result, VISTA has been identified as an appealing target for immunotherapy, and several VISTA inhibitors are currently in clinical and preclinical trials. In this review, the structural features and binding partners of VISTA are summarized, and we describe the latest developments of monoclonal antibodies and small molecules targeting VISTA as well as possible future directions for development of therapies targeting VISTA.

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