Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 6, Pages 1592-1595Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.02.020
Keywords
Acridine; Anticancer; Apoptosis; bcl-2; bcl-xL; Fluorescence polarization spectroscopy; Quinacrine
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Funding
- Spanish Ministry of Science and Innovation (MICINN) [BIO2004-998, BIO2007-60666, CSD2008-00005, BFU2005-09141]
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From the screening of a unique collection of 880 off-patent small organic molecules, we have found that quinacrine inhibits the interaction between a BH3 domain-derived peptide and the antiapoptotic protein Bcl-xL. Nuclear magnetic resonance spectroscopy confirmed that quinacrine binds to the hydrophobic groove that Bcl-xL uses for interacting with the BH3 domain of proapoptotic proteins. This activity can contribute to the anticancer activity of quinacrine. (C) 2009 Elsevier Ltd. All rights reserved.
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