2. Academic Validation
  3. A novel arginine methyltransferase inhibitor with cellular activity

A novel arginine methyltransferase inhibitor with cellular activity

  • Bioorg Med Chem Lett. 2007 Aug 1;17(15):4150-3. doi: 10.1016/j.bmcl.2007.05.088.
Astrid Spannhoff 1,  Rospita Machmur,  Ralf Heinke,  Patrick Trojer,  Ingo Bauer,  Gerald Brosch,  Roland Schüle,  Wolfgang Hanefeld,  Wolfgang Sippl,  Manfred Jung
Affiliations

Affiliation

  • 1 Institute of Pharmaceutical Sciences, Albert-Ludwigs-University of Freiburg, Germany.
PMID: 17570663 DOI: 10.1016/j.bmcl.2007.05.088
Abstract

Via virtual screening we identified a thioglycolic amide as an arginine methyltransferase (PRMT) inhibitor and tested it and related compounds against the Fungal PRMT RmtA and human PRMT1. Compound RM65 was the most potent druglike inhibitor (IC(50)-PRMT1: 55.4 microM) and showed histone hypomethylation in HepG2 cells. Docking studies proposed binding at the substrate and SAM cofactor binding pocket. It may serve as a lead for further PRMT inhibitors useful for the treatment for hormone dependent cancers.

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