Thursday, February 21, 2013
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of the first potent and selective inhibitor of a methyllysine-binding domain
suggests this class of epigenetic proteins could be targeted with small
molecules. In vitro, the lead compound, UNC1215,
inhibited the interaction of lethal(3)
malignant brain tumor-like 3
with a methylated peptide, with an IC50 value of 40 nM and at
least 50-fold selectivity over other proteins in the family. In cell culture,
UNC1215 blocked the interaction between L3MBTL3 and a methyllysine-dependent,
protein-binding partner. Next steps include screening for small molecule
inhibitors of additional methyllysine-binding proteins, including tumor
protein p53 binding protein 1 (TP53BP1;
SciBX 6(7); doi:10.1038/scibx.2013.178
Published online Feb. 21, 2013
status not applicable
James, L.I. et al. Nat.
published online Jan. 6, 2013;
Contact: Stephen V. Frye, The University of North Carolina
at Chapel Hill Eshelman School of Pharmacy, Chapel Hill, N.C.
Contact: Cheryl H. Arrowsmith, University of Toronto,
Toronto, Ontario, Canada
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