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Epigenetic, methyllysine-binding protein inhibitors

Identification 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 (L3MBTL3) 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; 53BP1) and chromobox homolog 7

SciBX 6(7); doi:10.1038/scibx.2013.178
Published online Feb. 21, 2013

Unpatented; licensing status not applicable

James, L.I. et al. Nat. Chem. Biol.;
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