期刊
PLOS ONE
卷 7, 期 8, 页码 -出版社
PUBLIC LIBRARY SCIENCE
DOI: 10.1371/journal.pone.0043278
关键词
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资金
- Hong Kong Baptist University [FRG2/10-11/008, FRG2/11-12/009]
- Environment and Conservation Fund (ECF) [3/2010]
- Centre for Cancer and Inflammation Research, School of Chinese Medicine (CCIR-SCM, HKBU)
- Research Fund for the Control of Infectious Diseases [RFCID/11101212]
- Research Grants Council [HKBU/201811]
- University of Macau [MYRG091(Y1-L2)-ICMS12-LCH, MYRG121(Y1-L3)-ICMS12-LCH]
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.
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