Description
Tranilastisaninhibitoroftransientreceptorpotentialvanilloid2(TRPV2)channelsandPDGFRs;itisalsoamastcellstABIlizer.Tranilastexhibitsanti-allergic,anti-fibrotic,immunomodulatory,anti-angiogenic,anti-metastatic,andanticancerchemotherapeuticactivities.Inanimalmodelsoffibrosis,tranilastinhibitsmastcellfiltrationanddecreaseslevelsofα-SMA,collagenI,fibronectin,stemcellfactor,andc-kit.Inotheranimalmodels,thiscompounddecreasesallograftrejectionandinducesTcellanergybyincreasingexpressionofp21andp51,decreasinglevelsofIL-2,andstimulatingcellcyclearrest.Incellularandanimalmodelsofbreastcancer,tranilastinducesG1/Sphasecellcyclearrest,decreaseslevelsofTGF-β1andendoglin,increaseslevelsofp53andactivationofcaspase3andPARP,andinhibitscellmigration,cellproliferation,andtumorgrowth.Invitro,tranilastinhibitsVEGF-andFGF-inducedcellproliferation,migration,andtubeformation.
References
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