Description
TamibaroteneisanagoNISTatretinoicacidreceptors(RARs)andisselectiveprimarilyforRARα/β.Tamibaroteneexhibitsneuroprotective,cognitionenhancing,immunomodulatory,andanticancerchemotherapeuticbenefits.Tamibaroteneupregulatestropomysin-relatedkinaseBandgrowth-associatedprotein43,inducingneuronaldifferentiation.Invivo,tamibaroteneactivatestheADAM10-Notch-Hes5signalingpathway,inhibitingdeteriorationofworkingmemoryandimprovingcognitivedeficitsindementiaandAlzheimer’sdisease.TamibarotenealsopreventsdecreasesinacetylcholineanddecreasessecretionofinflammatorycytokinesandanxietyinmodelsofAlzheimer’sdisease.Tamibarotenedecreasesiron-inducedoxidativestressinvivo,decreasingbloodglucoselevelsandhepaticironcontent.Inanimalmodelsofvasculitis,thiscompoundinhibitsneutrophilmigration,ROSproduction,andphosphorylationofERK1/2andp38.Tamibarotenealsoexhibitsimmunomodulatoryeffectsinanimalmodelsofgraft-versus-hostdisease(GVHD)andexperimentalautoimmuneencephalitis(EAE),alteringTh1andTh17responses.Additionally,tamibarotenemayinhibitcellgrowthinleukemiacellsandinducepartialregressionoftumorsinanimalmodelsofcancer.
References
KitaokaK,ShimizuN,OnoK,etal.TheretinoicacidreceptoragonistAm80increaseshippocampalADAM10inagedSAMP8mice.Neuropharmacology.2013Sep;72:58-65.PMID:23624141
YoshikawaO,EbataY,TsuchiyaH,etal.Aretinoicacidreceptoragonisttamibarotenesuppressesironaccumulationintheliver.Obesity(SilverSpring).2013Jan;21(1):E22-5.PMID:23404745.
MiyabeC,MiyabeY,MiuraNN,etal.Am80,aretinoicacidreceptoragonist,amelioratesmurinevasculitisthroughthesuppressionofneutrophilmigrationandactivation.ArthritisRheum.2013Feb;65(2):503-12.PMID:23203767.
FukasawaH,NakagomiM,YamagataN,etal.Tamibarotene:acandidateretinoiddrugforAlzheimer"sdisease.BiolPharmBull.2012;35(8):1206-12.PMID:22863914.
NishimoriH,MaedaY,TeshimaT,etal.SyntheticretinoidAm80ameliorateschronicgraft-versus-hostdiseasebydown-regulatingTh1andTh17.Blood.2012Jan5;119(1):285-95.PMID:22077062.
ShiohiraH,KitaokaA,ShirasawaH,etal.Am80inducesneuronaldifferentiationinahumanneuroblastomaNH-12cellline.IntJMolMed.2010Sep;26(3):393-9.PMID:20664956.
KlemannC,RaveneyBJ,KlemannAK,etal.SyntheticretinoidAM80inhibitsTh17cellsandamelioratesexperimentalautoimmuneencephalomyelitis.AmJPathol.2009Jun;174(6):2234-45.PMID:19389933.
