作者: G.S Chetrite , J.R Pasqualini
DOI: 10.1016/S0960-0760(01)00046-2
关键词: Aromatase 、 Sulfatase 、 Nomegestrol acetate 、 Medrogestone 、 Internal medicine 、 Promegestone 、 Endocrinology 、 Estrogen 、 Tibolone 、 Chemistry 、 Sulfotransferase
摘要: Abstract Human breast cancer tissue contains all the enzymes (estrone sulfatase, 17β-hydroxysteroid dehydrogenase, aromatase) involved in last steps of estradiol biosynthesis. This also sulfotransferase for formation biologically inactive estrogen sulfates. In years, it was demonstrated that various progestins (promegestone, nomegestrol acetate, medrogestone), as well tibolone and its metabolites are potent inhibitors sulfatase dehydrogenase activities. It shown medrogestone, promegestone or can stimulate activity local production All these data, addition to numerous agents, which block aromatase action, lead new concept selective enzyme modulators (SEEM), largely apply tissue. The exploration other active agents trials with patients, showing an inhibitory effect on a stimulatory sulfotransferase, will provide possibility treatment this disease.