Ligands playing musical chairs with G-quadruplex DNA: A rapid and simple displacement assay for identifying selective G-quadruplex binders

Ligands playing musical chairs with G-quadruplex DNA: A rapid and simple displacement assay for identifying selective G-quadruplex binders
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DOI:
10.1016/j.biochi.2008.02.019
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发表时间:
2008-08-01
期刊:
影响因子:
3.9
通讯作者:
Teulade-Fichou, M. -R
Teulade-Fichou, M. -R
中科院分区:
生物学3区
文献类型:
--
作者:
Monchaud, D.;Allain, C.;Teulade-Fichou, M. -R

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We report here the details of G4-FlD (G-quadruplex fluorescent intercalator displacement), a simple method aiming at evaluating quadruplex-DNA binding affinity and quadruplex-over duplex-DNA selectivity of putative ligands. This assay is based on the loss of fluorescence upon displacement of thiazole orange from quadruplex- and duplex-DNA matrices. The original protocol was tested using various quadruplex- and duplex-DNA targets, and with a wide panel of G-quadruplex ligands belonging to different families (i.e. from quinacridines to metallo-organic ligands) likely to display various binding modes. The reliability of the assay is further supported by comparisons with FRET-melting and ESI-MS assays. (C) 2008 Elsevier Masson SAS. All rights reserved.