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• W1963137324 abstract "Galeterone (Gal) is a first-in-class multi-target oral small molecule that will soon enter pivotal phase III clinical trials in castration resistant prostate cancer (CRPC) patients. Gal disrupts androgen receptor (AR) signaling via inhibition of CYP17, AR antagonism and AR degradation. Resistance to current therapy is attributed to up-regulation of full-length AR (fAR), splice variants AR (AR-Vs) and AR mutations. The effects of gal and VNPT55 were analyzed on f-AR and AR-Vs (AR-V7/ARv567es) in LNCaP, CWR22Rv1 and DU145 (transfected with AR-Vs) human PC cells in vitro and CRPC tumor xenografts. Galeterone/VNPT55 decreased fAR/AR-V7 mRNA levels and implicates Mdm2/CHIP enhanced ubiquitination of posttranslational modified receptors, targeting them for proteasomal degradation. Gal and VNPT55 also induced significant apoptosis in PC cells via increased Bax/Bcl2 ratio, cytochrome-c release with concomitant cleavage of caspase 3 and PARP. More importantly, gal and VNPT55 exhibited strong in vivo anti-CRPC activities, with no apparent host toxicities. This study demonstrate that gal and VNPT55 utilize cell-based mechanisms to deplete both fAR and AR-Vs. Importantly, the preclinical activity profiles, including profound apoptotic induction and inhibition of CRPC xenografts suggest that these agents offer considerable promise as new therapeutics for patients with CRPC and those resistant to current therapy." @default.
• W1963137324 created "2016-06-24" @default.
• W1963137324 creator A5007287283 @default.
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• W1963137324 creator A5042775164 @default.
• W1963137324 creator A5049666672 @default.
• W1963137324 date "2015-07-14" @default.
• W1963137324 modified "2023-10-01" @default.
• W1963137324 title "Galeterone and VNPT55 induce proteasomal degradation of AR/AR-V7, induce significant apoptosis via cytochrome c release and suppress growth of castration resistant prostate cancer xenografts<i>in vivo</i>" @default.
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• W1963137324 doi "https://doi.org/10.18632/oncotarget.4578" @default.
• W1963137324 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4695001" @default.
• W1963137324 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26196320" @default.
• W1963137324 hasPublicationYear "2015" @default.
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