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1、Ru-IndoloquinolineComplexasaSelectiveandEffectiveHumanTelomericG-quadruplexBinder#YuHuijuan*5101520(SchoolofChemicalEngineeringandLightIndustry,GuangdongUniversityofTechnolog,)Abstract:IndoloquinolineanditsderivativeshavebeenreportedtobeakindofefficientG-quad
2、ruplexbinderandhavebeenfoundtointeractpreferentiallytointramolecularG-qudruplexandinhibittelomeraseactivityinhumanK562cellsandSW620cells.Incontrasttoindoloquinolinederivatives,muchlessisknownaboutthemetalcomplexbasedonindoloquinolineoritsderivative.Inthisreport
3、,westudiedtheinteractionofrutheniumcomplex[Ru(bpy)2(itatp)]2+whichcontaingindoloquinolinemoietywithhumantelomericG-quadruplexDNA(Telo22)andc-mycG-quadruplexDNA(Pu27)byUV-visible(UV-Vis),fluorescencespectroscopy,fluorescentintercalatordisplacement(FID),thermalde
4、naturationstudiesandCDspectroscopy.Theresultssuggestthat[Ru(bpy)2(itatp)]2+displaysastrongπ-πstackinginteractionwithhumantelomericG-quadruplexwithahighbindingconstant(~107M-1),butjustexhibitsslightbindingaffinitytoc-mycG-quadruplex,thusshowingsignificantselecti
5、vityoverhumantelomericG-quadruplex.TheCDtitrationresultsindicatethat[Ru(bpy)2(itatp)]2+couldeffectivelyconvertTelo22intoantiparallelG-quadruplexconformation,whileinthec-mycG-quadruplexcase,insteadofpromotingPu27tofoldintoG-quadruplex,[Ru(bpy)2(itatp)]2+destroys
6、theparallelG-quadruplexstructureofPu27.Keywords:G-quadruplex;Telomere;Rutheniumcomplex;Indoloquinoline0IntroductionDNAistheprincipalgeneticmoleculeinbiologicalsystems,andisknowntoadoptrighthandedduplexstructureB-DNA.However,thestructureofDNAispolymorphic,anumb
7、erofalternativestructuresnon-BDNA,suchasZ-DNA,hairpins,cruciform,andquadruplex,have2530354045beenidentifiedandfoundtobeunstableandmutagenic[1-3].Amongthesenon-Bconformations,G-quadruplexDNAhasreceivedconsiderableattention.G-quadruplexstructuresareadoptedbyguan
8、ine-richsequencesandconsistofπ-πstackedplanesoffourguanosinescyclicallyboundtoeachotherviaeighthydrogenbondsaccordingtotheHoogsteenmotif[4-5].TheG-quadruplexformingsequences
