Galeterone is effective at preventing binding of [3H]-R1881 to the mutant LNCaP AR (T877A) and to T575A mutant AR in PC3 cells with IC50 values of 845 nM and 454 nM, respectively. The effects on AR significantly reduce cellular phospho-4EBP1 levels. Galeterone potently inhibits the proliferation of LNCaP and LAPC4 cells in the with IC50 values of 2.6 μM and 4 μM, respectively. Galeterone induces the endoplasmic reticulum s.tress response resulting in down-regulation of cyclin D1 protein expression and cyclin E2 mRNA in vitro. Galeterone is a selective CYP17 inhibitor and AR (androgen receptor) antagonist
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PMID: # 27174722 Bogner, J. et al. 2017. J. Steroid Biochem. Mol. Biol. 166: 45-53.