Thursday, February 21, 2013
This week in techniques
Publication and contact
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
All contents Copyright © 1993-2016 BioCentury Publications, Inc. ALL RIGHTS RESERVED. All use of this Web Site and its contents is governed by the BioCentury User Agreement
. The contents of this Web Site are protected under U.S. and foreign copyright and intellectual property laws, and no part of this Web Site or its contents may be photocopied, reproduced or retransmitted in any form without the written consent of BioCentury, which may be requested from Reprints/Permissions
. BioCentury®; The Bernstein Report on BioBusiness™; The BioCentury 100™; The Clear Route to ROI™; Because Real Intelligence is Hard to Find™; BCIQ™; and BioPharma's Knowledge Center™; are trademarks of BioCentury Publications, Inc., P.O. Box 1246, San Carlos, CA 94070. SciBX® and SciBX: Science-Business eXchange® are trademarks of Nature America, Inc. that are jointly used by BioCentury Publications, Inc. and Nature America, Inc.
Thanks for purchasing this article.
Please bookmark this url for future reference.
We have also sent you a confirming e-mail with a receipt and this same url for your
close [ X ]