revealing

期刊名称：ACSPharmacology&TranslationalScience

作者：JonKObst,JunWang,KunzhongJian,ms,

年份：2019年

期号：第XXXX期

关键词：UDP-glucuronosyltransfera(UGT2B);ralaniten;drug

resistance;androgenreceptor

摘要：Inhibitionofandrogenreceptor(AR)isthemainstaytreatmentfor

ten(formallyEPI-002)preventsARtranscriptional

activitybybindingtoitsN-terminaldomain(NTD)whichisntialfor

tenacetate(EPI-506)thetri-acetatepro-drugof

ralaniten,remainstheonlyAR-NTDinhibitortohaveenteredclinicaltrials

(NCT02606123).Whilewelltolerated,thetrialwasultimatelyterminateddueto

discoveredthat

-term

treatmentofprostatecancercellswithralanitenresultsinupregulationofUGT2B

sprovedaufulmodelwith

whichtofacilitatethedevelopmentofmorepotent...

内容由中国教育图书进出口有限公司引进

RevealingMetabolicLiabilitiesofRalanitenTo

EnhanceNovelAndrogenReceptorTargeted

Therapies