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1、PERSPECTIVESG-quadruplex-formingsequencesimmedi-OPINIONatelyupstreamanddownstreamofthetranscriptionstartsiteinproliferation-TargetingG‑quadruplexesassociatedgenesthroughbioinformaticsstudies(seebelow).Notably,G-quadruplexesingenepromoters:anovelarefoundinthegenepromotersofawiderangeofge
2、nesthatareimportantincellanticancerstrategy?signalling,whichhaverepresentativesfromthesixhallmarksofcancer11.AswellastranscriptionfactorssuchasMYC,whichShankarBalasubramanian,LaurenceH. HurleyandStephenNeidleisanundruggabletargetattheproteinlevelowingtoitsshorthalf-lifeandunstructuredAb
3、stract
4、G-quadruplexesarefour-strandedDNAstructuresthatareover-nature12,othertargetsofparticularinterestrepresentedingenepromoterregionsandareviewedasemergingtherapeuticincludethesmallGTPaseKRASandthetargetsinoncology,astranscriptionalrepressionofoncogenesthroughstabilizationreceptortyro
5、sinekinaseKIT,whichisaclini-ofthesestructurescouldbeanovelanticancerstrategy.Manygenepromotercallyvalidateddrugtargetfortreatinggastrointestinalstromaltumours13.G-quadruplexeshavephysicochemicalpropertiesandstructuralcharacteristicsthatConsequently,fromadrug-mightmakethemdruggable,andth
6、eirstructuraldiversitysuggeststhatahighdevelopmentperspective,ifrobustdegreeofselectivitymightbepossible.Here,wedescribetheevidenceforstrategiesfortherapeuticallytargetingG-quadruplexesingenepromotersanddiscusstheirpotentialastherapeutictargets,genepromoterG-quadruplexstructuresaswellas
7、progressinthedevelopmentofstrategiestoharnessthispotentialthroughcouldbeestablished,theirpotentialmightbebroad,perhapsevenanalogoustointerventionwithsmall-moleculeligands.targetingcurrentmajordrugtargetfamilies,suchasproteinkinases.Moreover,themajorDNAwasthefirstdefinedtargetforanti-Asa
8、resultofresearchontelomericadvantageoftargetingG-quadruplexes,cancerdrugs(forahistoricalperspective,G-quadruplexesandthecellularconse-comparedwithpreviouslytargetedfamiliesseeREF. 1).However,withtheadventofquencesoftargetingthemwithsmallmole-ofDNAstructures,isthattheyarediscret
