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  • Title: Spectroscopic and biological studies of phenanthroline compounds: selective recognition of gene-promoter G-quadruplex DNAs preferred over duplex DNA.
    Author: Wang L, Wei C.
    Journal: Chem Biodivers; 2013 Jun; 10(6):1154-64. PubMed ID: 23776031.
    Abstract:
    G-Quadruplex DNA formed in the promoter regions of proto-oncogenes would block the transcription process and eventually suppress the development of tumors, so compounds that stabilize G-quadruplex DNA are potential antitumor drugs. This article describes the interactions of three phenanthroline compounds, a-c, with proto-oncogene c-kit2 and c-myc G-quadruplex DNAs by means of polymerase chain reaction (PCR) stop assay, fluorescence resonance energy transfer melting (FRET melting) assay, fluorescence indicator displacement (FID) assay, UV/VIS absorption, fluorescence, and circular dichroism (CD) spectroscopies. All three compounds displayed selectivity for the G-quadruplex over duplex, with binding constants (Ka) for the both quadruplexes varying from 0.49×10⁶ to 3.32×10⁶ M⁻¹ (4.1- to 33.2-fold specificity). Compounds a, b, and c were potential stabilizers for the c-kit2 G-quadruplex with the melting-temperature increase (ΔTm) values of 12-15°. CD Spectra indicated that a-c disrupted the structure of c-kit2 G-quadruplex, whereas no significant change was observed for c-myc G-quadruplex.
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