Literature DB >> 24900829

Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.

Kanchan Devkota1, Brian Lohse2, Qing Liu3, Ming-Wei Wang3, Dan Stærk2, Jens Berthelsen4, Rasmus Prætorius Clausen2.   

Abstract

A series of analogues of the natural product sinefungin lacking the amino acid moiety was synthesized and probed for their ability to inhibit EHMT1 and EHMT2. This study led to inhibitors 3b and 4d of methyltransferase activity of EHMT1 and EHMT2 and it demonstrates that such analogues constitute an interesting scaffold to develop selective methyltransferase inhibitors. Surprisingly, the inhibition was not competitive toward AdoMet.

Entities:  

Keywords:  EHMT1; EHMT2; Sinefungin; methyltransferase inhibitors

Year:  2014        PMID： 24900829      PMCID： PMC4027773          DOI： 10.1021/ml4002503

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


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