Research progress of protein arginine methyltransferase 5 inhibitors

ZHAN Kangning; QUAN Xu; HUANG Zhangjian; ZHAO Liwen

doi:10.11665/j.issn.1000-5048.20210315

Journal of China Pharmaceutical University > 2021 > 52(3): 371-378. > DOI: 10.11665/j.issn.1000-5048.20210315

ZHAN Kangning, QUAN Xu, HUANG Zhangjian, ZHAO Liwen. Research progress of protein arginine methyltransferase 5 inhibitors[J]. Journal of China Pharmaceutical University, 2021, 52(3): 371-378. DOI: 10.11665/j.issn.1000-5048.20210315

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Research progress of protein arginine methyltransferase 5 inhibitors

1.
Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009
2.
Nanjing Sanhome Pharmaceutical Co.,Ltd., Nanjing 210038, China

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Received Date: May 17, 2020
Revised Date: April 20, 2021

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Abstract

Abstract

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.
- PRMT5,
- small molecular inhibitors,
- epigenetics,
- arginine methylation,
- antitumor target

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References (47)

References

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