Description
BexaroteneisaretinoidcompoundthatbindsandactivatesretinoidXreceptors(RXRs)andisapprovedtotreatcutaneousTcelllymphoma.Bexarotenedisplaysawidevarietyofbeneficialactivities,suchasanticancerchemotherapeutic,anti-hyperlipidemic,andneuroprotectiveproperties.Bexarotenehasshownpre-clinicalandclinicalefficacyintreatmentofothercancers,increasingapoptosisandinducingtumorregressioninvitroandinvivo.Bexarotene’sactivationofRXRsalsoresultsinactivationofPPARαsignaling,decreasingtriglyceridelevelsandincreasingHDLcholesterollevelsinvivo.ThiscompoundinteractswithnuclearhormonereceptorNurr1-RXRheterodimers,reversingbehavioraldeficitsinducedby6-OHDAinratmodelsofParkinson’sdisease.Additionally,bexaroteneactivationofRXRsinducesApoE-dependentclearanceofamyloid-β(Aβ)peptidesandplaques,reversingcognitivedeficitsinanimalmodelsofAlzheimer’sdisease.