Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 5, Issue 4, Pages 293-297Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml4002503
Keywords
Sinefungin; methyltransferase inhibitors; EHMT1; EHMT2
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Funding
- University of Copenhagen
- Danish Cancer Society
- University of Copenhagen Programme of Excellence
- Ministry of Science and Technology of China [2009ZX09302-001, 2012ZX09304011, 2013ZX09507002]
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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 Ado Met.
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