NCIt definition : An orally bioavailable adrenal steroid analogue with potential antineoplastic activity.
Androstane steroid HE3235 appears to bind the androgen receptor (AR), down-regulating
anti-apoptotic genes, such as Bcl-2, while increasing the expression of pro-apoptotic
genes, such as caspases. In vitro and in vivo studies indicate that this agent inhibits
androstenediol-dependent LNCaP cell tumor growth. In addition, HE3235 may potentiate
chemotherapeutic agents by down-regulating ABCG2, the gene encoding the multi-drug
resistant (MDR) protein MDR2.;