Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/6518
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Title: Discovery of a natural product-like c-myc G-quadruplex DNA groove-binder by molecular docking
Authors: Ma, DL
Chan, DSH
Fu, WC 
He, HZ
Yang, H
Yan, SC
Leung, CH
Issue Date: 17-Aug-2012
Source: PLoS one, 17 Aug., 2012, v. 7, no. 8, e43278, p. 1-8
Abstract: The natural product-like carbamide (1) has been identified as a stabilizer of the c-myc G-quadruplex through high-throughput virtual screening. NMR and molecular modeling experiments revealed a groove-binding mode for 1. The biological activity of 1 against the c-myc G-quadruplex was confirmed by its ability to inhibit Taq polymerase-mediated DNA extension and c-myc expression in vitro, demonstrating that 1 is able to control c-myc gene expression at the transcriptional level presumably through the stabilization of the c-myc promoter G-quadruplex. Furthermore, the interaction between carbamide analogues and the c-myc G-quadruplex was also investigated by in vitro experiments in order to generate a brief structure-activity relationship (SAR) for the observed potency of carbamide 1.
Keywords: Promoter region
Down-regulation
Ligand
Recognition
Identification
Stabilization
Transcription
Target
Publisher: Public Library of Science
Journal: PLoS one 
EISSN: 1932-6203
DOI: 10.1371/journal.pone.0043278
Rights: © 2012 Ma et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
The website of Creative Commons Attribution 3.0 Unported (CC by 3.0) is located at <http://creativecommons.org/licenses/by/3.0/>
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