Enhancing endothelial progenitor cell function through selective estrogen receptor modulation: a potential approach...

Area of Science:

• Pharmacology
• Cardiovascular Medicine
• Endocrinology

Background:

• Estrogen receptors (ER) are key targets for pharmacological intervention.
• Menopausal hormone therapy (MHT) for cardiovascular health has risks, including stroke.
• Selective estrogen receptor modulators (SERMs) were developed to improve MHT safety and efficacy.

Purpose of the Study:

• To explore the connection between SERMs and endothelial progenitor cell (EPC) biology.
• To identify novel strategies for cardiovascular risk reduction targeting specific cells and tissues.

Main Methods:

• Review of existing evidence on MHT and SERMs (tamoxifen, raloxifene, lasofoxifene).
• Examination of fundamental research on estrogen actions in the cardiovascular system, focusing on EPCs.
• Analysis of ER-isoform selectivity and ER biology.

Main Results:

• Current SERMs do not consistently demonstrate superior cardiovascular efficacy or safety over MHT.
• Lasofoxifene reduced cardiovascular events but increased venous thromboembolic events.
• Endothelial progenitor cells are identified as crucial targets of estrogen in the cardiovascular system.

Conclusions:

• Targeting specific cells like EPCs may enhance the safety of ER modulators.
• Understanding ER biology and isoform selectivity is crucial for developing safer and more effective ER modulators for cardiovascular risk reduction.