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Updated: Aug 22, 2025

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
Published on: May 2, 2025
PD-L1 small-molecule modulators: A new hope in epigenetic-based multidrug cancer therapy?
Clemens Zwergel1, Rossella Fioravanti1, Antonello Mai2
1Department of Drug Chemistry and Technologies, Department of Excellence 2018-2022, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy.
Abstract:
Programmed death-ligand 1 (PD-L1) is an immune checkpoint protein the overexpression of which results in an inhibitory signal that induces T cell exhaustion responsible for immune escape in tumors. Immunotherapy strategies targeting the PD-L1 pathway have achieved remarkable success in treating various types of cancer. More recently, numerous advances in understanding the complex PD-L1 biology have been made, and the first small-molecule inhibitors have been described in the literature. In this review, we highlight the most promising recent advances in understanding the complex regulation mechanisms focusing on small-molecule modulators, which could be used in rational therapy combinations with other epigenetic chemotherapeutic agents.
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