Title of article
A novel arginine methyltransferase inhibitor with cellular activity
Author/Authors
Astrid Spannhoff، نويسنده , , Rospita Machmur، نويسنده , , Ralf Heinke، نويسنده , , Patrick Trojer، نويسنده , , Ingo Bauer، نويسنده , , Gerald Brosch، نويسنده , , Roland Schüle، نويسنده , , Wolfgang Hanefeld، نويسنده , , Wolfgang Sippl، نويسنده , , Manfred Jung، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
4150
To page
4153
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 (IC50-PRMT1: 55.4 μM) 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.
Keywords
Arginine methyltransferase , PRMT , Virtual screening , Histone methyltransferase , Docking , chromatin
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798384
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