Research progress of protein arginine methyltransferase 5 inhibitors / 中国药科大学学报

@#Protein arginine methyltransferases, which proceed the post-translational modification of both histones and non-histones, play an important role in many biological pathways. Protein arginine methyltransferase 5 (PRMT5) is a major enzyme responsible for symmetric di-methylation of arginine residues and has been suggested as a potential therapeutic target for tumors.In the past decade,the discovery and development of PRMT5 inhibitors have become one of the most important research fields.This article introduces the structure and biochemical function of PRMT5 and its correlation with cancer reviews, the binding modes and biological data of PRMT5 inhibitors under development, and discusses the clinical application potential of PRMT5 inhibitors in the treatment of cancer.

Gene Regulation by Histone Arginine Modifications / 生物化学与生物物理进展

Methylation of histone by protein arginine methyltransferases (PRMTs) plays an important role in gene regulation. PRMT1- and PRMT4-catalyzed methyl-arginine is involved in transcription activation, while PRMT5- and PRMT6-catalyzed methyl-arginine is associated with transcription repression. Histone arginine methylation can be dynamically regulated in vivo, and methyl-arginine is demethylated by "arginine demethylase". Here, the most recent progresses in the methylation studies of histone arginine were summarized.