Anticancer Activity of a Novel Selective CYP17A1 Inhibitor in Preclinical Models of Castrate-Resistant Prostate Cancer

Toren P, et al., 14(1):59-69, Mol Cancer Ther, 2015

This article reports the preclinical results of a novel small molecule CYP17A1 enzyme inhibitor called VT-464. Particularly, the anticancer activity of VT-464 was compared with that of ABI in prostate cancer cell lines and in xenograft models. The reversible interaction between small molecules and the androgen receptor was evaluated using an Octet RED system. The authors used a biotinylated androgen receptor (produced using the AviTag technology), which was captured onto super Streptavidin biosensors as the ligand. The results suggest a better performance by VT-464 as compared to ABI.

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