Description
2-MethoxyestrADIolisametaboliteofestradiolthatexhibitsanti-angiogenic,vasodilatory,antihypertensive,anti-fibrotic,anticancerchemotherapeuticandchemopreventiveactivities.2-Methoxyestradiolalsodisplaysantimitoticactivity,bindingthecolchicinesiteoftubulinandstABIlizingmicrotubulepolymerization.Thiscompounddecreasestumorgrowth,VEGFexpression,andangiogenesisinanimalmodelsofhepatocellularcarcinomaandpreventsinitialdevelopmentoftumorsinanimalmodelsofprostatecancer.Inhypertensiverates,2-methoxyestradioldecreasesmeanarterialbloodpressure.Additionally,thiscompoundinhibitsTGF-β3-inducedfibrosisinvitro,decreasingexpressionofcollagen,PAI-1,CTGF,andα-SMAandpreventingphosphorylationofSmad2/3.
References
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