Literature DB >> 19632837

Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies.

Honghe Wan1, Tram Huynh, Suhong Pang, Jieping Geng, Wayne Vaccaro, Michael A Poss, George L Trainor, Matthew V Lorenzi, Marco Gottardis, Lata Jayaraman, Ashok V Purandare.   

Abstract

Hit to Lead optimization and SAR development led to the identification of the potent and selective benzo[d]imidazole inhibitor (17b) of Co-activator Associated Arginine Methyltransferase (CARM1).

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Year:  2009        PMID: 19632837     DOI: 10.1016/j.bmcl.2009.07.040

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


  21 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

Review 2.  Chromatin proteins and modifications as drug targets.

Authors:  Kristian Helin; Dashyant Dhanak
Journal:  Nature       Date:  2013-10-24       Impact factor: 49.962

3.  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 4.  Chemical biology of protein arginine modifications in epigenetic regulation.

Authors:  Jakob Fuhrmann; Kathleen W Clancy; Paul R Thompson
Journal:  Chem Rev       Date:  2015-05-13       Impact factor: 60.622

Review 5.  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

Review 6.  Recent progress in developing selective inhibitors of protein methyltransferases.

Authors:  H Ümit Kaniskan; Jian Jin
Journal:  Curr Opin Chem Biol       Date:  2017-06-26       Impact factor: 8.822

Review 7.  Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11.

Authors:  David F Tough; Huw D Lewis; Inmaculada Rioja; Matthew J Lindon; Rab K Prinjha
Journal:  Br J Pharmacol       Date:  2014-11       Impact factor: 8.739

8.  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

9.  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

10.  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

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