Inhibition of steroid sulphatase activity in endometriotic implants by 667 COUMATE: a potential new therapy
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Inhibition of steroid sulphatase activity in endometriotic implants by 667 COUMATE: a potential new therapy.
BACKGROUND Local biosynthesis of estrogens is thought to be important for the maintenance and growth of endometriotic implants. In addition to the formation of estrogen via the aromatase pathway, steroid sulphatase (STS), which is responsible for the hydrolysis of estrogen sulphates, may be an important source of estrogens in endometriosis. METHODS Eutopic and ectopic endometrial samples from...
متن کاملAdvances in Brief In Vivo Inhibition of Estrone Sulfatase Activity and Growth of Nitrosomethylurea- induced Mammary Tumors by 667 COUMATE
The development of potent steroid sulfatase inhibitors is an important new therapeutic strategy for the treatment of postmenopausal women with breast cancer. A series of tricyclic coumarin sulfamates were synthesized, and their inhibitory properties were examined in vitro and in vivo. In a placental microsomal assay system, 667 COUMATE emerged as the most potent inhibitor with an IC50 of 8 nM. ...
متن کاملIn vivo inhibition of estrone sulfatase activity and growth of nitrosomethylurea-induced mammary tumors by 667 COUMATE.
The development of potent steroid sulfatase inhibitors is an important new therapeutic strategy for the treatment of postmenopausal women with breast cancer. A series of tricyclic coumarin sulfamates were synthesized, and their inhibitory properties were examined in vitro and in vivo. In a placental microsomal assay system, 667 COUMATE emerged as the most potent inhibitor with an IC50 of 8 nM. ...
متن کاملPhase I study of STX 64 (667 Coumate) in breast cancer patients: the first study of a steroid sulfatase inhibitor.
PURPOSE Inhibition of steroid sulfatase (STS), the enzyme responsible for the hydrolysis of steroid sulfates, represents a potential novel treatment for postmenopausal women with hormone-dependent breast cancer. Estrone and DHEA are formed by this sulfatase pathway and can be converted to steroids (estradiol and androstenediol, respectively), which have potent estrogenic properties. EXPERIMEN...
متن کاملRecognising placental steroid sulphatase deficiency
bad, with variable results in between. Amputation of a digit is sometimes thought to produce a quicker return to work for the patient than replantation, but this is not borne out by published results."' The outlook in the leg is less clear. Functional results are often poor if a leg is replanted. Nevertheless, filleting may produce useful soft tissue which may be used as a vascularised free tra...
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ژورنال
عنوان ژورنال: Human Reproduction
سال: 2007
ISSN: 0268-1161,1460-2350
DOI: 10.1093/humrep/dem308