Steroid Sulfatase: Molecular Biology, Regulation, and Inhibition
March 2005
in “
Endocrine Reviews
”
steroid sulfatase STS steroid sulfates active steroids hormone-dependent cancers breast cancer prostate cancer estrogen receptor-positive tumors STS inhibitors steroidal inhibitors nonsteroidal inhibitors phenol sulfamate ester 667 COUMATE X-linked ichthyosis immune response cognitive function hormone formation breast tumors prostate tumors estrogen receptor-positive breast cancer phenol sulfamate ester inhibitors
TLDR The enzyme steroid sulfatase is linked to breast cancer and other conditions, and inhibitors are being developed for treatment.
The document from 2005 provides a comprehensive overview of steroid sulfatase (STS), an enzyme involved in the conversion of steroid sulfates into active steroids, which has implications for various physiological and pathological conditions, including hormone-dependent cancers like breast and prostate cancer. It was found that STS expression is increased in breast tumors and serves as a prognostic indicator for relapse-free survival, particularly in estrogen receptor-positive tumors. The enzyme's crystal structure has been resolved, but its regulation remains poorly understood. The development of STS inhibitors, both steroidal and nonsteroidal, has been pursued due to the enzyme's role in tumor growth, with irreversible inhibitors containing a phenol sulfamate ester showing promise. One such inhibitor, 667 COUMATE, has entered phase I clinical trials for breast cancer treatment. STS activity is also significant in skin conditions such as X-linked ichthyosis and may play roles in immune response and cognitive function. The document also discusses the importance of STS in hormone formation and the development of potent inhibitors with potential therapeutic applications beyond oncology.
