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Updated: Mar 19, 2026

Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
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Function of G-Protein-Coupled Estrogen Receptor-1 in Reproductive System Tumors

Hongyan Qian1, Jingxiu Xuan1, Yuan Liu1

  • 1Department of Rheumatology and Clinical Immunology, The First Affiliated Hospital of Xiamen University, Xiamen 361003, China.

Journal of Immunology Research
|June 18, 2016
PubMed

Insights

G-protein-coupled estrogen receptor-1 (GPER-1) promotes estrogen-related cancers via non-ER pathways but also shows potential as a therapeutic target. GPER-1 activation can inhibit cancer cell proliferation, highlighting its complex role.

Area of Science:

  • Oncology
  • Molecular Biology
  • Endocrinology

Background:

  • G-protein-coupled estrogen receptor-1 (GPER-1), also known as GPR30, is a novel estrogen receptor.
  • GPER-1 mediates estrogen receptor signaling in various cell types.
  • Estrogen-related cancers are influenced by GPER-1 activity.

Purpose of the Study:

  • To summarize the characteristics and complex functions of GPER-1 in cancers.
  • To explore GPER-1's role in promoting estrogen-related cancer progression.
  • To investigate GPER-1 as a potential therapeutic target in oncology.

Main Methods:

  • Literature review of GPER-1 functions in cancer.
  • Analysis of signaling pathways involved in GPER-1 activity (MAPK, PI3K, PLC).
  • Examination of clinical evidence linking GPER-1 to estrogen resistance.

Main Results:

  • GPER-1 activation promotes estrogen-related cancer progression via non-classic estrogen receptor (ER) dependent pathways.
  • GPER-1 is associated with estrogen resistance in cancer patients.
  • Preclinical studies show GPER-1 agonist G-1 inhibits cancer cell proliferation.

Conclusions:

  • GPER-1 exhibits complex, dual roles in cancer, promoting progression yet offering therapeutic potential.
  • GPER-1 represents a promising novel therapeutic target for estrogen-related cancers.
  • Further research into GPER-1 signaling is crucial for developing effective cancer treatments.

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