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G-protein-coupled estrogen receptor as a new therapeutic target for treating coronary artery disease

Guichun Han1, Richard E White1

  • 1Guichun Han, Women's Health Division, Michael E DeBakey Institute, Department of Physiology and Pharmacology, College of Veterinary Medicine and Biomedical Sciences, Texas A and M University, College Station, TX 77843, United States.

World Journal of Cardiology
|July 1, 2014
PubMed

Insights

Selective activation of the G-protein-coupled estrogen receptor (GPER) in coronary arteries shows promise for treating coronary heart disease (CHD). This approach may increase blood flow and reduce disease consequences while avoiding estrogen therapy side effects.

Area of Science:

  • Cardiovascular Biology
  • Endocrinology
  • Pharmacology

Background:

  • Coronary heart disease (CHD) is a leading cause of mortality.
  • Estrogen therapy for CHD has potential benefits but significant side effects and risks.
  • Estrogen therapy may be detrimental to cardiovascular health in postmenopausal women.

Purpose of the Study:

  • To review the current understanding of G-protein-coupled estrogen receptor (GPER) activation in coronary arteries.
  • To explore the potential of selective GPER activation as a therapeutic strategy for CHD.
  • To discuss the signaling mechanisms involved in GPER activation within coronary arteries.

Main Methods:

  • Review of existing scientific literature on GPER expression and function in coronary arteries.
  • Analysis of studies investigating the effects of GPER agonists on coronary vasodilation.
  • Examination of research on GPER's role in coronary smooth muscle cell proliferation and migration.

Main Results:

  • G-protein-coupled estrogen receptor (GPER) is expressed in coronary endothelium and smooth muscle.
  • GPER activation leads to coronary artery dilation.
  • GPER activation inhibits coronary smooth muscle cell proliferation and migration.

Conclusions:

  • Selective GPER activation offers a potential therapeutic avenue for treating coronary heart disease (CHD).
  • Targeting GPER may increase coronary blood flow and mitigate atherosclerotic disease progression.
  • Understanding GPER signaling could lead to novel CHD therapies with improved safety profiles compared to traditional estrogen therapy.

Keywords:
AtherosclerosisCoronary arteriesEstrogenG-1G-protein-coupled estrogen receptor

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