SCREENING AND DETERMINATION OF KINETIC-PARAMETERS OF AROMATASE INHIBITORS USING HUMAN GENITAL SKIN FIBROBLASTS

The screening of aromatase inhibitors using human genital skin fibrobl asts (GSF) in culture is described. Using this system the selectivity in detecting inhibition compares well with that for human fall-term pl acenta as a source of enzyme. IC50 and K(i) values may be determined u sing GSF and the ranking of a group of known inhibitors tested compare s with that using placental enzyme. The advantages of this method are that the tissue is readily available and the long term freezing of via ble cells allows a ready supply of material for repeated experiments.