A Chloroacetamidine-Based Inactivator of Protein Arginine Methyltransferase 1: Design, Synthesis, and In Vitro and In Vivo Evaluation

被引：35

作者：

Obianyo, Obiamaka ^{[1
]}

Causey, Corey P. ^{[1
]}

Osborne, Tanesha C. ^{[1
]}

Jones, Justin E. ^{[1
]}

Lee, Young-Ho ^{[2
]}

Stallcup, Michael R. ^{[2
]}

Thompson, Paul R. ^{[1
]}

机构：

[1] Univ S Carolina, Dept Chem & Biochem, Columbia, SC 29208 USA

[2] Univ So Calif, Dept Biochem, Los Angeles, CA 90089 USA

来源：

CHEMBIOCHEM | 2010年 / 11卷 / 09期

关键词：

CI-amidine; enzymes; inhibitors; protein arginine methyltransferase; transcription; SUBSTRATE PEPTIDES; DEIMINASE; 4; METHYLATION; BINDING; PRMT1; PAD4;

D O I：

10.1002/cbic.201000209

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

(Chemical Equation Presented) Protein arginine methyltransferases (PRMTs) catalyze the post-translational methylation of arginine residues. PRMT1 is the predominant mammalian isozyme and is responsible for generating the majority of the asymmetrically dimethylated arginine found in vivo. Herein, we describe the most potent PRMT1 inhibitor, C21, described to date. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：1219 / 1223

页数：5

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