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Updated: Jul 30, 2025

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Advances in Medicinal Chemistry of Estrogen-related Receptor Alpha (ERRα) Inverse Agonists

Haibin Zhang1, Yongli Du1, Yong Zheng1

  • 1School of Chemistry & Chemical Engineering, Qilu University of Technology (Shandong Academy of Sciences), Jinan, 250353, China.

Current Topics in Medicinal Chemistry
|May 16, 2023
PubMed

Insights

Estrogen-related receptor alpha (ERRα) is a target for triple-negative breast cancer (TNBC) treatment. ERRα inverse agonists show potential in inhibiting tumor growth by blocking ERRα expression and downstream signaling pathways.

Area of Science:

  • Molecular Endocrinology
  • Oncology
  • Drug Discovery

Background:

  • Estrogen-related receptor alpha (ERRα) is overexpressed in breast cancer, particularly triple-negative breast cancer (TNBC), correlating with poor prognosis.
  • ERRα overexpression is linked to increased tumor cell migration and angiogenesis via downstream targets like VEGF and WNT11.
  • Upstream oncogenic factors such as mTOR, HER2, and PI3K regulate ERRα expression.

Conclusions:

  • ERRα inverse agonists represent a promising therapeutic strategy for TNBC.
  • Further research into structure-activity relationships is crucial for optimizing ERRα inverse agonists.
  • Development of novel ERRα inverse agonists could lead to effective treatments for TNBC.
Keywords:
Breast cancerERRalphaERRalpha inverse agonistsInverse agonistic activitySignaling pathwaysTNBC

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