Recent advances in targeting protein arginine methyltransferase enzymes in cancer therapy.
Recent advances in targeting protein arginine methyltransferase enzymes in cancer therapy.
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DOI：
10.1080/14728222.2018.1474203
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发表时间：
2018-06
影响因子：
5.8
通讯作者：
Baiocchi RA
中科院分区：
文献类型：
--
作者：
Smith E;Zhou W;Shindiapina P;Sif S;Li C;Baiocchi RA
表观遗传学领域的探索揭示了精氨酸甲基转移酶（PRMT）蛋白家族在多种疾病状态中的不同作用。这些发现导致了特异性抑制剂的开发，并发现了几类新的药物，这些药物有可能治疗良性和恶性疾病。我们提供了PRMT酶在健康和恶性细胞中的作用的概述，突出精氨酸甲基化在与癌症发病机制相关的特定途径中的作用。此外，我们还描述了PRMT的结构和催化活性，并讨论了精氨酸甲基转移酶家族特定成员的新型小分子抑制剂的作用机制。随着PRMT生物学领域的发展，越来越清楚的是，这类酶与维持正常的生理过程以及疾病的发病机制高度相关。我们讨论了PRMT抑制剂作为一种广泛的药物的潜在影响，包括多效性效应，脱靶效应，需要更详细的PRMT为中心的相互作用，最后，靶向这类酶的潜力在临床开发的实验性治疗癌症。
Exploration in the field of epigenetics has revealed the diverse roles of the arginine methyltransferase (PRMT) family of proteins in multiple disease states. These findings have led to the development of specific inhibitors and discovery of several new classes of drugs with potential to treat both benign and malignant conditions. We provide an overview on the role of PRMT enzymes in healthy and malignant cells, highlighting the role of arginine methylation in specific pathways relevant to cancer pathogenesis. Additionally, we describe structure and catalytic activity of PRMT and discuss the mechanisms of action of novel small molecule inhibitors of specific members of the arginine methyltransferase family. As the field of PRMT biology advances, it’s becoming clear that this class of enzymes is highly relevant to maintaining normal physiologic processes as well and disease pathogenesis. We discuss the potential impact of PRMT inhibitors as a broad class of drugs, including the pleiotropic effects, off target effects the need for more detailed PRMT-centric interactomes, and finally, the potential for targeting this class of enzymes in clinical development of experimental therapeutics for cancer.
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影响因子：
2.6
作者：
Cheng H;Qin Y;Fan H;Su P;Zhang X;Zhang H;Zhou G
通讯作者：
Zhou G
影响因子：
8.8
作者：
Blanc, Romeo Sebastien;Vogel, Gillian;Richard, Stephane
通讯作者：
Richard, Stephane
DOI：
10.1039/jr9510002492
发表时间：
1951-01-01
期刊：
JOURNAL OF THE CHEMICAL SOCIETY
影响因子：
--
作者：
ANGYAL, SJ;WARBURTON, WK
通讯作者：
WARBURTON, WK
影响因子：
11.4
作者：
Chevillard-Briet, M;Trouche, D;Vandel, L
通讯作者：
Vandel, L
影响因子：
10.5
作者：
Ceschin, Danilo Guillermo;Walia, Mannu;Gronemeyer, Hinrich
通讯作者：
Gronemeyer, Hinrich