Histone lysine methyltransferase SET8 is a novel therapeutic target for cancer treatment. Issue 10 (October 2021)

• Record Type: Journal Article
• Authors: Yang, Chao; Wang, Kai; Zhou, YingTang; Zhang, Shao-Lin
• Is Part Of: Drug discovery today. Volume 26:Issue 10(2021)
• Page Start: 2423
• Page End: 2430
• Publication Date: 2021-10
• Subjects: Histone methylation -- SET8 inhibitor -- Epigenetic modification -- Cancer therapy; Drugs -- Design -- Periodicals; Drugs -- Research -- Periodicals; 615.1
• DOI: 10.1016/j.drudis.2021.05.004
• Languages: English
• ISSNs: 1359-6446

Abstract

Graphical abstract: Highlights: SET8 inhibition is a promising strategy for cancer therapy. Detailed pathophysiology functions of SET8 is described. Providing hints for the future development of SET8 inhibitors. Abstract: SET8 is the only lysine methyltransferase that can specifically monomethylate the histone H4K20. SET8-mediated protein modifications are largely involved in the regulation of cell cycle, DNA repair, gene transcription, cell apoptosis, and other vital physiological processes. The aberrant expression of SET8 is closely linked to the proliferation, invasion, metastasis, and prognosis of a variety of cancers. As a consequence, targeting SET8 could be an appealing strategy for cancer therapy. In this article, we introduce the molecular structure of SET8, followed by summarizing its roles in various biological pathways. Crucially, we highlight the potential functions of SET8 in tumors, as well as progress in the development of SET inhibitors for cancer treatment.