Steroid sulfatase inhibitors: promising new tools for breast cancer therapy?
Abstract
Inhibition of aromatase is currently well-established as the major treatment option of hormone-dependent breast cancer in postmenopausal women. However, despite the effects of aromatase inhibitors in both early and metastatic breast cancer, endocrine resistance may cause relapses of the disease and progression of metastasis. Thus, driven by the success of manipulating the steroidogenic enzyme aromatase, several alternative enzymes involved in steroid synthesis and metabolism have recently been investigated as possible drug targets. One of the most promising targets is the steroid sulfatase (STS) which converts steroid sulfates like estrone sulfate (E1S) and dehydroepiandrosterone sulfate (DHEAS) to estrone (E1) and dehydroepiandrosterone (DHEA), respectively. Estrone and DHEA may thereafter be used for the synthesis of more potent estrogens and androgens that may eventually fuel hormone-sensitive breast cancer cells. The present review summarizes the biology behind steroid sulfatase and its inhibition, the currently available information derived from basic and early clinical trials in breast cancer patients, as well as ongoing research. Article from the Special Issue on Targeted Inhibitors.
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The potential of STS inhibition has been evaluated in promising clinical trials.
“The potential of STS inhibition has been evaluated in promising clinical trials (Geisler et al., 2011, Purohit and Foster, 2012, Thomas and Potter, 2015).”
From Intracrine androgen biosynthesis, metabolism and action revisited (2018) · cites this paper as Geisler et al., 2011
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The Regulation of Steroid Action by Sulfation and Desulfation
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“The potential of STS inhibition has been evaluated in promising clinical trials (Geisler et al., 2011; Purohit and Foster, 2012; Thomas and Potter, 2015).”
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Self-citation
- Authors
- Geisler, J., Sasano, H., Chen, S., & Purohit, A.
- Affiliations
- University of Oslo (NO)
- Tohoku University (JP)
- Beckman Research Institute (US)
- Hammersmith Hospital (GB)
- Corresponding author
- Geisler, Jürgen
- Venue
- The Journal of Steroid Biochemistry and Molecular Biology
- Publisher
- Elsevier BV
- Published
- 2011-05
- Volume
- 125
- Issue
- 1-2
- Pages
- 39-45
- ISSN
- 0960-0760 (ISSN-L)
- OpenAlex
- W2044695707
- Cited by
- 55
- References
- 55
- Citations by year
- 2026: 2 · 2024: 1 · 2022: 6 · 2021: 3 · 2020: 3 · 2019: 2 · 2018: 5 · 2017: 4 · 2016: 5 · 2015: 6 · 2014: 3 · 2013: 8 · 2012: 3
- FWCI
- 0.64
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- Locations
- The Journal of Steroid Biochemistry and Molecular Biology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Breast Cancer Treatment Studies
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer, Lipids, and Metabolism
- Keywords
- steroid sulfatase inhibitors, steroid sulfatase, breast cancer, endocrine therapy resistance, aromatase inhibitors, estrone sulfate, dehydroepiandrosterone sulfate, steroid metabolism, hormone-dependent breast cancer, targeted therapy
- MeSH terms
- Androgens, Breast Neoplasms, Clinical Trials as Topic, Enzyme Inhibitors, Estrogens, Female, Humans, Molecular Structure, Steryl-Sulfatase, Aromatase Inhibitors
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