PD-L1 small-molecule modulators: A new hope in epigenetic-based multidrug cancer therapy?. Issue 2 (February 2023)

• Record Type: Journal Article
• Authors: Zwergel, Clemens; Fioravanti, Rossella; Mai, Antonello
• Is Part Of: Drug discovery today. Volume 28:Issue 2(2023)
• Publication Date: 2023-02
• Subjects: immunotherapy -- PD-L1 -- epigenetics -- cancer -- therapy escape -- multitarget approach; Drugs -- Design -- Periodicals; Drugs -- Research -- Periodicals; 615.1
• DOI: 10.1016/j.drudis.2022.103435
• Languages: English
• ISSNs: 1359-6446

Abstract

Highlights: Short digest on the latest updates regarding immunotherapy with a focus on PD-L1. Summary of the recent advances in the field of small molecule PD-L1 modulators. Overview of the growing interest in rational therapy combinations of PD-L1 modulators with epidrugs. 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.