Histone Methyltransferases as Therapeutic Targets for Kidney Diseases

Front Pharmacol. 2019 Dec 6;10:1393. doi: 10.3389/fphar.2019.01393.

Chao Yu ¹, Shougang Zhuang ¹ ²

Affiliations

1 Department of Nephrology, Shanghai East Hospital, Tongji University School of Medicine, Shanghai, China.
2 Department of Medicine, Rhode Island Hospital and Alpert Medical School, Brown University, Providence, RI, United States.

PMID: 31866860 DOI: 10.3389/fphar.2019.01393

Abstract

Emerging evidence has demonstrated that epigenetic regulation plays a vital role in gene expression under normal and pathological conditions. Alterations in the expression and activation of histone methyltransferases (HMTs) have been reported in preclinical models of multiple kidney diseases, including acute kidney injury, chronic kidney disease, diabetic nephropathy, polycystic kidney disease, and renal cell carcinoma. Pharmacological inhibition of these Enzymes has shown promise in preclinical models of those renal diseases. In this review, we summarize recent knowledge regarding expression and activation of various HMTs and their functional roles in some kidney diseases. The preclinical activity of currently available HMT inhibitors and the mechanisms of their actions are highlighted.

Keywords

chronic kidney diseases; epigenetic regulations; expression; histone methyltransferases; histone modification.

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