Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms

The protein arginine methyltransferase 5 (PRMT5) as the major type II arginine methyltransferase catalyzes the mono- and symmetric dimethylation of arginine residues in both histone and non-histone proteins. Recently, increasing evidence has demonstrated that PRMT5 plays an indispensable role in the...

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Autores principales:	Yingqing Chen, Xiaomin Shao, Xiangge Zhao, Yuan Ji, Xiaorong Liu, Peixuan Li, Mingyu Zhang, Qianqian Wang
Formato:	article
Lenguaje:	EN
Publicado:	Elsevier 2021
Materias:	PRMT5 Cancer Inhibitors Histone methylation Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/21949dc41c81459f896375b78c91734d
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spelling	oai:doaj.org-article:21949dc41c81459f896375b78c91734d2021-11-14T04:28:51ZTargeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms0753-332210.1016/j.biopha.2021.112252https://doaj.org/article/21949dc41c81459f896375b78c91734d2021-12-01T00:00:00Zhttp://www.sciencedirect.com/science/article/pii/S0753332221010362https://doaj.org/toc/0753-3322The protein arginine methyltransferase 5 (PRMT5) as the major type II arginine methyltransferase catalyzes the mono- and symmetric dimethylation of arginine residues in both histone and non-histone proteins. Recently, increasing evidence has demonstrated that PRMT5 plays an indispensable role in the occurrence and development of various human cancers by promoting the cell proliferation, invasion, and migration. It has become a promising and valuable target in the cancer epigenetic therapy. This review is to summarize the clinical significance of PRMT5 in the cancers such as lung cancer, breast cancer and colorectal cancer, and the drug discovery targeting PRMT5. Importantly, the existing PRMT5 inhibitors representing different molecular mechanisms, and their pharmacological effect, mechanism of action and biological affinity are analyzed. Clinical status, current problems and future perspective of PRMT5 inhibitors for the treatment of cancers are also discussed, all of which provides crucial help for the future discovery of PRMT5 targeted drugs for cancer treatment.Yingqing ChenXiaomin ShaoXiangge ZhaoYuan JiXiaorong LiuPeixuan LiMingyu ZhangQianqian WangElsevierarticlePRMT5CancerInhibitorsHistone methylationTherapeutics. PharmacologyRM1-950ENBiomedicine & Pharmacotherapy, Vol 144, Iss , Pp 112252- (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	PRMT5 Cancer Inhibitors Histone methylation Therapeutics. Pharmacology RM1-950
spellingShingle	PRMT5 Cancer Inhibitors Histone methylation Therapeutics. Pharmacology RM1-950 Yingqing Chen Xiaomin Shao Xiangge Zhao Yuan Ji Xiaorong Liu Peixuan Li Mingyu Zhang Qianqian Wang Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms
description	The protein arginine methyltransferase 5 (PRMT5) as the major type II arginine methyltransferase catalyzes the mono- and symmetric dimethylation of arginine residues in both histone and non-histone proteins. Recently, increasing evidence has demonstrated that PRMT5 plays an indispensable role in the occurrence and development of various human cancers by promoting the cell proliferation, invasion, and migration. It has become a promising and valuable target in the cancer epigenetic therapy. This review is to summarize the clinical significance of PRMT5 in the cancers such as lung cancer, breast cancer and colorectal cancer, and the drug discovery targeting PRMT5. Importantly, the existing PRMT5 inhibitors representing different molecular mechanisms, and their pharmacological effect, mechanism of action and biological affinity are analyzed. Clinical status, current problems and future perspective of PRMT5 inhibitors for the treatment of cancers are also discussed, all of which provides crucial help for the future discovery of PRMT5 targeted drugs for cancer treatment.
format	article
author	Yingqing Chen Xiaomin Shao Xiangge Zhao Yuan Ji Xiaorong Liu Peixuan Li Mingyu Zhang Qianqian Wang
author_facet	Yingqing Chen Xiaomin Shao Xiangge Zhao Yuan Ji Xiaorong Liu Peixuan Li Mingyu Zhang Qianqian Wang
author_sort	Yingqing Chen
title	Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms
title_short	Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms
title_full	Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms
title_fullStr	Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms
title_full_unstemmed	Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms
title_sort	targeting protein arginine methyltransferase 5 in cancers: roles, inhibitors and mechanisms
publisher	Elsevier
publishDate	2021
url	https://doaj.org/article/21949dc41c81459f896375b78c91734d
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Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms

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