Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 7, Pages 2103-2105Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.02.069
Keywords
Protein arginine methyltransferases; Small-molecule inhibitors; S-Adenosylmethionine; Methylation; Epigenetics
Categories
Funding
- Medical Research Council [G0700840]
- University of Nottingham
- MRC [G0700840] Funding Source: UKRI
- Medical Research Council [G0700840] Funding Source: researchfish
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Prototype inhibitors of protein arginine methyltransferases (PRMTs) have been constructed by attaching guanidine functionality via a variable linker to non-reactive amine analogues of the cellular co-factor (S)-adenosyl methionine (AdoMet). Potent inhibition of PRMT1 (IC50 of similar to 3-6 mu M) combined with weak inhibition of the lysine methyltransferase SET7 (similar to 50% of activity at 100 mu M) was observed for two such compounds. (C) 2010 Elsevier Ltd. All rights reserved.
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