Literature DB >> 19836951

1,2-Diamines as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).

Eric Therrien1, Guillaume Larouche, Sukhdev Manku, Martin Allan, Natalie Nguyen, Sylvia Styhler, Marie-France Robert, Anne-Christine Goulet, Jeffrey M Besterman, Hannah Nguyen, Amal Wahhab.   

Abstract

We have identified the N(1)-benzyl-N(2)-methylethane-1,2-diamine unit as a substitute for the (S)-alanine benzylamide moiety for the design of co-activator associated arginine methyltransferase 1 (CARM1) inhibitors. The potency of these inhibitors is in the same order of magnitude as their predecessors and their clearance, volume of distribution, and half lives were greatly improved.

Entities:  

Mesh：

Substances：

Year:  2009        PMID： 19836951     DOI： 10.1016/j.bmcl.2009.09.110

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  16 in total

Review 1.  Small Molecule Inhibitors of Protein Arginine Methyltransferases.

Authors:  Hao Hu; Kun Qian; Meng-Chiao Ho; Y George Zheng
Journal:  Expert Opin Investig Drugs       Date:  2016-02-16       Impact factor: 6.206

2.  Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1).

Authors:  H Ü Kaniskan; M S Eram; J Liu; D Smil; M L Martini; Y Shen; V Santhakumar; P J Brown; C Arrowsmith; M Vedadi; J Jin
Journal:  Medchemcomm       Date:  2016-07-13       Impact factor: 3.597

Review 3.  Inhibitors of Protein Methyltransferases and Demethylases.

Authors:  H Ümit Kaniskan; Michael L Martini; Jian Jin
Journal:  Chem Rev       Date:  2017-03-24       Impact factor: 60.622

4.  Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity.

Authors:  Donghang Cheng; Sergio Valente; Sabrina Castellano; Gianluca Sbardella; Roberto Di Santo; Roberta Costi; Mark T Bedford; Antonello Mai
Journal:  J Med Chem       Date:  2011-06-13       Impact factor: 7.446

5.  Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.

Authors:  Yudao Shen; Magdalena M Szewczyk; Mohammad S Eram; David Smil; H Ümit Kaniskan; Renato Ferreira de Freitas; Guillermo Senisterra; Fengling Li; Matthieu Schapira; Peter J Brown; Cheryl H Arrowsmith; Dalia Barsyte-Lovejoy; Jing Liu; Masoud Vedadi; Jian Jin
Journal:  J Med Chem       Date:  2016-09-15       Impact factor: 7.446

6.  Xenoestrogens regulate the activity of arginine methyltransferases.

Authors:  Donghang Cheng; Mark T Bedford
Journal:  Chembiochem       Date:  2010-12-17       Impact factor: 3.164

7.  Identification of small-molecule enhancers of arginine methylation catalyzed by coactivator-associated arginine methyltransferase 1.

Authors:  Sabrina Castellano; Astrid Spannhoff; Ciro Milite; Fabrizio Dal Piaz; Donghang Cheng; Alessandra Tosco; Monica Viviano; Abdellah Yamani; Agostino Cianciulli; Marina Sala; Vincent Cura; Jean Cavarelli; Ettore Novellino; Antonello Mai; Mark T Bedford; Gianluca Sbardella
Journal:  J Med Chem       Date:  2012-11-02       Impact factor: 7.446

8.  A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.

Authors:  Elayne Chan-Penebre; Kristy G Kuplast; Christina R Majer; P Ann Boriack-Sjodin; Tim J Wigle; L Danielle Johnston; Nathalie Rioux; Michael J Munchhof; Lei Jin; Suzanne L Jacques; Kip A West; Trupti Lingaraj; Kimberly Stickland; Scott A Ribich; Alejandra Raimondi; Margaret Porter Scott; Nigel J Waters; Roy M Pollock; Jesse J Smith; Olena Barbash; Melissa Pappalardi; Thau F Ho; Kelvin Nurse; Khyati P Oza; Kathleen T Gallagher; Ryan Kruger; Mikel P Moyer; Robert A Copeland; Richard Chesworth; Kenneth W Duncan
Journal:  Nat Chem Biol       Date:  2015-04-27       Impact factor: 15.040

9.  A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.

Authors:  Mohammad S Eram; Yudao Shen; Magdalena Szewczyk; Hong Wu; Guillermo Senisterra; Fengling Li; Kyle V Butler; H Ümit Kaniskan; Brandon A Speed; Carlo Dela Seña; Aiping Dong; Hong Zeng; Matthieu Schapira; Peter J Brown; Cheryl H Arrowsmith; Dalia Barsyte-Lovejoy; Jing Liu; Masoud Vedadi; Jian Jin
Journal:  ACS Chem Biol       Date:  2015-12-08       Impact factor: 5.100

10.  Targets in epigenetics: inhibiting the methyl writers of the histone code.

Authors:  Julianne M Yost; Ilia Korboukh; Feng Liu; Cen Gao; Jian Jin
Journal:  Curr Chem Genomics       Date:  2011-08-22
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.