Screening and Determination of Kinetic Parameters of Aromatase Inhibitors Using Human Genital Skin Fibroblasts

Abstract

The screening of aromatase inhibitors usiing human genital skin fibroblasts (GSF) in culture is described. Using this system the selectivity in detecting inhibition compares well with that for human full-term placenta as a source of enzyme. IC₅₀ and K_i values may be determined using GSF and the ranking of a group of known inhibitors tested compares with that using placental enzyme. The advantages of this method are that the tissue is readily available and the long term freezing of viable cells allows a ready supply of material for repeated experiments.

Key Words: :

• Aromatase inhibitors
• placental aromatase
• genital skin fibroblasts
• aromatase screening