Description
XAV-939inhibitstankyrasesandwntpathwaysignaling.XAVexhibitsanti-fibroticactivityandshowspotentialanticancerchemotherapeuticbenefitwhenco-admiNISTeredwithothercompounds.XAV-939decreasesnuclearaccumulationofβ-cateninanddecreasesc-myclevels,decreasingbleomycin-induceddermalthickening.Inbothinvitroandinvivomodelsofcancer,thiscompoundreversesresistancetoPI3KandAktinhibitors.
References
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DistlerA,DelochL,HuangJ,etal.InactivationoftankyrasesreducesexperimentalfibrosisbyinhibitingcanonicalWntsignalling.AnnRheumDis.2013Sep1;72(9):1575-80.PMID:23148305.
TenbaumSP,Ordóñez-MoránP,PuigI,etal.β-cateninconfersresistancetoPI3KandAKTinhibitorsandsubvertsFOXO3atopromotemetastasisincoloncancer.NatMed.2012Jun;18(6):892-901.PMID:22610277.