Description
Tirapazamineisananticancerchemotherapeuticcompoundcurrentlyinclinicaltrialsco-admiNISTeredwithcisplatinorrADIationasapotentialtreatmentforseveralcancers.TirapazamineinhibitsDNAtopoisomeraseIIαandmodulatesreplicationproteinA(RPA),inhibitingDNAreplication.TirapazaminealsoformsDNAdamagingfreeradicals,inducingsingle-anddouble-strandedDNAbreaks.Additionally,tirapazamineinhibitsexpressionofHIF-1α,potentiallythroughmodulationofeukaryoticinitiationfactoreIF2αphosphorylation.Thiscompoundinducesapoptosisinneuroblastomacells,decreasingthemitochondrialmembranepotentialandlevelsofglutathione;thiseffectmaybep53-dependent.