Evidence That the G Protein-Coupled Membrane Receptor GPR30 Contributes to the Cardiovascular Actions of Estrogen

Although female protection from cardiovascular diseases declines with the fall in circulating sex hormones experienced during menopause, clinical trials in older women fail to demonstrate beneficial effects for hormone replacement therapy. The recent discovery of GPR30, a membrane-bound estrogen receptor that is structurally and functionally unique from the steroid receptors ER alpha and ER beta, has unveiled additional signaling pathways by which estrogen may influence cardiovascular health. This review takes an organ-based approach to assess the expression and function of GPR30 in the cardiovascular system. We concluded that although the current literature does suggest a cardiovascular role for GPR30, additional exploration is necessary to fully elucidate the estrogenic actions mediated by this novel receptor. (Gend Med. 2011;8:343-354) (C) 2011 Elsevier HS Journals, Inc. All rights reserved.