PMID- 23776031 OWN - NLM STAT- MEDLINE DCOM- 20140117 LR - 20130618 IS - 1612-1880 (Electronic) IS - 1612-1872 (Linking) VI - 10 IP - 6 DP - 2013 Jun TI - Spectroscopic and biological studies of phenanthroline compounds: selective recognition of gene-promoter G-quadruplex DNAs preferred over duplex DNA. PG - 1154-64 LID - 10.1002/cbdv.201200341 [doi] AB - 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 0.49x10(6) to 3.32x10(6) 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 (DeltaTm) values of 12-15 degrees . 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. CI - Copyright (c) 2013 Verlag Helvetica Chimica Acta AG, Zurich. FAU - Wang, Lihua AU - Wang L AD - Key Laboratory of Chemical Biology and Molecular Engineering of Ministry of Education, Institute of Molecular Science, Shanxi University, Taiyuan 030006, PR China. FAU - Wei, Chunying AU - Wei C LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Switzerland TA - Chem Biodivers JT - Chemistry & biodiversity JID - 101197449 RN - 0 (Phenanthrolines) RN - 0 (Proto-Oncogene Proteins c-myc) RN - 9007-49-2 (DNA) RN - EC 2.7.10.1 (Proto-Oncogene Proteins c-kit) SB - IM MH - Circular Dichroism MH - DNA/*chemistry/metabolism MH - Fluorescence Resonance Energy Transfer MH - *G-Quadruplexes MH - Phenanthrolines/*chemistry/metabolism MH - Proto-Oncogene Proteins c-kit/genetics MH - Proto-Oncogene Proteins c-myc/genetics MH - Spectrophotometry, Ultraviolet MH - Transition Temperature EDAT- 2013/06/19 06:00 MHDA- 2014/01/18 06:00 CRDT- 2013/06/19 06:00 PHST- 2012/10/05 00:00 [received] PHST- 2013/06/19 06:00 [entrez] PHST- 2013/06/19 06:00 [pubmed] PHST- 2014/01/18 06:00 [medline] AID - 10.1002/cbdv.201200341 [doi] PST - ppublish SO - Chem Biodivers. 2013 Jun;10(6):1154-64. doi: 10.1002/cbdv.201200341.