Pyrazole inhibitors of coactivator associated arginine methyltransferase 1 (CARM1)

被引：69

作者：

Purandare, Ashok V. ^{[1
]}

Chen, Zhong ^{[1
]}

Huynh, Tram ^{[1
]}

Pang, Suhong ^{[1
]}

Geng, Jieping ^{[1
]}

Vaccaro, Wayne ^{[1
]}

Poss, Michael A. ^{[1
]}

Oconnell, Jonathan ^{[1
]}

Nowak, Kimberly ^{[1
]}

Jayaraman, Lata ^{[1
]}

机构：

[1] Bristol Myers Squibb Pharmaceut Res & Dev, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 15期

关键词：

coactivator associated arginine; methyltransferase; 1; CARM1; PRMT4; protein arginine methyltransferase;

D O I：

10.1016/j.bmcl.2008.06.026

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This study reports the identification and Hits to Leads optimization of inhibitors of coactivator associated arginine methyltransferase (CARM1). Compound 7b is a potent, selective inhibitor of CARM1. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：4438 / 4441

页数：4

共 16 条

[1] Regulation of transcription by a protein methyltransferase [J].

Chen, DG ;

Ma, H ;

Hong, H ;

Koh, SS ;

Huang, SM ;

Schurter, BT ;

Aswad, DW ;

Stallcup, MR .

SCIENCE, 1999, 284 (5423) :2174-2177

[2] Small molecule regulators of protein arginine methyltransferases [J].

Cheng, DH ;

Yadav, N ;

King, RW ;

Swanson, MS ;

Weinstein, EJ ;

Bedford, MT .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2004, 279 (23) :23892-23899

[3] The arginine methyltransferase CARM1 regulates the coupling of transcription and mRNA processing [J].

Cheng, Donghang ;

Cote, Jocelyn ;

Shaaban, Salam ;

Bedford, Mark T. .

MOLECULAR CELL, 2007, 25 (01) :71-83

[4] Control of CBP co-activating activity by arginine methylation [J].

Chevillard-Briet, M ;

Trouche, D ;

Vandel, L .

EMBO JOURNAL, 2002, 21 (20) :5457-5466

[5] CARM1 regulates proliferation of PC12 cells by methylating HuD [J].

Fujiwara, T ;

Mori, Y ;

Chu, DL ;

Koyama, Y ;

Miyata, S ;

Tanaka, H ;

Yachi, K ;

Kubo, T ;

Yoshikawa, H ;

Tohyama, M .

MOLECULAR AND CELLULAR BIOLOGY, 2006, 26 (06) :2273-2285

[6] Aberrant expression of CARM1, a transcriptional coactivator of androgen receptor, in the development of prostate carcinoma and androgen-independent status [J].

Hong, H ;

Kao, CH ;

Jeng, MH ;

Eble, JN ;

Koch, MO ;

Gardner, TA ;

Zhang, SB ;

Li, L ;

Pan, CX ;

Hu, ZQ ;

MacLennan, GT ;

Cheng, L .

CANCER, 2004, 101 (01) :83-89

[7] Protein arginine methyltransferases: Evolution and assessment of their pharmacological and therapeutic potential [J].

Krause, Christopher D. ;

Yang, Zhi-Hong ;

Kim, Young-Sun ;

Lee, Jin-Hyung ;

Cook, Jeffry R. ;

Pestka, Sidney .

PHARMACOLOGY & THERAPEUTICS, 2007, 113 (01) :50-87

[8] PABP1 identified as an arginine methyltransferase substrate using high-density protein arrays [J].

Lee, J ;

Bedford, MT .

EMBO REPORTS, 2002, 3 (03) :268-273

[9] Lipopolysaccharide-induced methylation of HuR, an mRNA-stabilizing protein, by CARM1 [J].

Li, HW ;

Park, SM ;

Kilburn, B ;

Jelinek, MA ;

Henschen-Edman, A ;

Aswad, DW ;

Stallcup, MR ;

Laird-Offringa, IA .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2002, 277 (47) :44623-44630

[10]

MAI A, 2008, J MED CHEM

← 1 2 →