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http://hdl.handle.net/10397/6518
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/> |
Appears in Collections: | Journal/Magazine Article |
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