1007872-70-9Relevant academic research and scientific papers
Phosphoramidate derivatives of hydroxysteroids as inhibitors of prostate-specific membrane antigen
Wu, Lisa Y.,Do, Jacinda C.,Kazak, Marat,Page, Helen,Toriyabe, Yoko,Anderson, Marc O.,Berkman, Clifford E.
, p. 281 - 284 (2008/09/16)
Prostate-specific membrane antigen (PSMA) is a membrane-bound cell surface peptidase which is over-expressed in prostate cancer cells. The enzymatic activities of PSMA are understood but the role of the enzyme in prostate cancer remains conjectural. We previously confirmed the existence of a hydrophobic binding site remote from the enzyme's catalytic center. To explore the specificity and accommodation of this binding site, we prepared a series of six glutamate-containing phosphoramidate derivatives of various hydroxysteroids (1a-1f). The inhibitory potencies of the individual compounds of the series were comparable to a simple phenylalkyl analog (8), and in all cases IC50 values were sub-micromolar. Molecular docking was used to develop a binding model for these inhibitors and to understand their relative inhibitory potencies against PSMA.
