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Published on: August 13, 2019
Developing Potential Endocrine Therapy Controlling Estradiol and DHT by Targeting 17β-HSD7 Against ER+ Breast Cancer
Ruixuan Wang1,2, Xiaoqiang Wang3, Peng Su1,2
1Axe Endocrinology and Nephrology, CHU de Québec Research Center, Université Laval, Quebec City, QC G1V 4G2, Canada.
Cells
|August 13, 2026
Summary
A novel inhibitor, INH7(464), targets 17β-HSD7 to block estrogen production in breast cancer. This new approach shows promise in reducing tumor size and offers a potential alternative to existing therapies facing resistance.
Area of Science:
- Oncology
- Endocrinology
- Biochemistry
Background:
- Breast cancer (BC) is a leading cancer in women, with endocrine therapies like SERMs and AIs improving outcomes.
- Significant resistance to current first-line endocrine therapies, particularly aromatase inhibitors (AIs), necessitates novel therapeutic strategies for estrogen-dependent BC.
Purpose of the Study:
- To investigate 17β-hydroxysteroid dehydrogenase type 7 (17β-HSD7) as a therapeutic target for estrogen-dependent breast cancer.
- To evaluate the efficacy of INH7(464), a novel 17β-HSD7 inhibitor, in preclinical models of breast cancer.
Main Methods:
- In vitro assessment of INH7(464)'s inhibitory activity against 17β-HSD7 (IC50 determination).
- Evaluation of INH7(464)'s effects on cell proliferation, cell cycle progression, and hormone levels (estradiol and dihydrotestosterone) in BC cell lines.
- In vivo studies using BC xenografts in mice to assess tumor growth inhibition and hormone level changes.
Main Results:
- INH7(464) demonstrated potent inhibition of 17β-HSD7 with an IC50 of 92 ± 8 nM, decreasing estradiol and restoring dihydrotestosterone levels.
- INH7(464) effectively inhibited breast cancer cell proliferation and induced G0/G1 cell cycle arrest.
- In vivo, INH7(464) significantly reduced tumor size by 49% and lowered estradiol levels in circulation and tumor tissue without observed cytotoxicity.
Conclusions:
- 17β-HSD7 is a viable therapeutic target for estrogen-dependent breast cancer.
- INH7(464) exhibits preclinical efficacy as a potential lead compound for treating breast cancer, addressing limitations of current therapies.
Keywords:
candidate compound for endocrine therapy against breast cancercell cycle arrestcytotoxicity and basic short-term in vivo toxicitydual control of sex hormonesefficacy of 17β-HSD7 inhibitors on xenograft tumor shrinkagefeedback control on enzyme expressionhERG inhibitionreductive 17β-hydroxysteroid dehydrogenases
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