Cited by 137Estrogen and related hormone effectsSteroid Chemistry and BiochemistryProstate Cancer Treatment and Research

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Steroid sulfatase inhibitors for estrogen- and androgen-dependent cancers

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Purohit, Atul, Foster, Paul A·2012·Journal of Endocrinology

DOI 10.1530/joe-11-0266

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Abstract

Estrogens and androgens are instrumental in the maturation of many hormone-dependent cancers. Consequently, the enzymes involved in their synthesis are cancer therapy targets. One such enzyme, steroid sulfatase (STS), hydrolyses estrone sulfate, and dehydroepiandrosterone sulfate to estrone and dehydroepiandrosterone respectively. These are the precursors to the formation of biologically active estradiol and androstenediol. This review focuses on three aspects of STS inhibitors: 1) chemical development, 2) biological activity, and 3) clinical trials. The aim is to discuss the importance of estrogens and androgens in many cancers, the developmental history of STS inhibitor synthesis, the potency of these compounds in vitro and in vivo and where we currently stand in regards to clinical trials for these drugs. STS inhibitors are likely to play an important future role in the treatment of hormone-dependent cancers. Novel in vivo models have been developed that allow pre-clinical testing of inhibitors and the identification of lead clinical candidates. Phase I/II clinical trials in postmenopausal women with breast cancer have been completed and other trials in patients with hormone-dependent prostate and endometrial cancer are currently active. Potent STS inhibitors should become therapeutically valuable in hormone-dependent cancers and other non-oncological conditions.

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Self-citation

Authors: Purohit, A., & Foster, P. A.
Affiliations: Hammersmith Hospital (GB)
ORCID: Foster, Paul A
Venue: Journal of Endocrinology
Publisher: Bioscientifica
Published: 2011-08-22
Volume: 212
Issue: 2
Pages: 99-110
ISSN: 0022-0795 (ISSN-L)
1479-6805
DOI: 10.1530/joe-11-0266
OpenAlex: W2143089038
Cited by: 126
References: 105
Citations by year: 2026: 3 · 2025: 3 · 2024: 2 · 2023: 7 · 2022: 5 · 2021: 8 · 2020: 5 · 2019: 12 · 2018: 11 · 2017: 11 · 2016: 14 · 2015: 12 · 2014: 16 · 2013: 11 · 2012: 6
FWCI: 1.11
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: Journal of Endocrinology (publishedVersion)
PubMed (publishedVersion)
University of Birmingham Research Portal (University of Birmingham) (submittedVersion)
Funders: Ipsen
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
Physical Sciences › Chemistry › Organic Chemistry › Steroid Chemistry and Biochemistry
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Prostate Cancer Treatment and Research
Keywords: steroid sulfatase inhibitors, steroid sulfatase, estrone sulfate, dehydroepiandrosterone sulfate, hormone-dependent tumors, breast cancer, prostate cancer, endometrial cancer, estrogen metabolism, androgen metabolism, drug development, clinical trials, postmenopausal women
MeSH terms: Androgens, Animals, Breast Neoplasms, Enzyme Inhibitors, Estrogens, Female, Humans, Male, Neoplasm Proteins, Neoplasms, Hormone-Dependent, Prostatic Neoplasms, Receptors, Androgen, Receptors, Estrogen, Antineoplastic Agents, Hormonal, Steryl-Sulfatase, Aromatase Inhibitors, Molecular Targeted Therapy

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Steroid sulfatase inhibitors for estrogen- and androgen-dependent cancers

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