Androgen use

Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[ 18 F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp 741 to Cys). [1] Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. [2]

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Androgen use

androgen use

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