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E-mail: jarterbu nmsu. Estrogens are critical mediators of multiple and diverse physiologic effects throughout the body in both sexes, including the reproductive, cardiovascular, endocrine, nervous, and immune systems. As such, alterations in estrogen function play important roles in many diseases and pathophysiological conditions including cancer , exemplified by the lower prevalence of many diseases in premenopausal women.
Although both receptor families can initiate rapid cell signaling and transcriptional regulation, the nuclear receptors are traditionally associated with regulating gene expression, whereas GPCRs are recognized as mediating rapid cellular signaling.
Estrogen-activated pathways are not only the target of multiple therapeutic agents e. Because of the existence of multiple estrogen receptors with overlapping ligand specificities, expression patterns, and signaling pathways, the roles of the individual receptors with respect to the diverse array of endogenous and exogenous ligands have been challenging to ascertain. In this review, we describe the history and characterization of GPER over the past 15 years focusing on the pharmacology of steroidal and nonsteroidal compounds that have been employed to unravel the biology of this most recently recognized estrogen receptor.
The pharmacology and physiology of estrogen and its receptors are particularly complex Dahlman-Wright et al. Although estrogens are recognized predominantly for their function in female mammalian reproduction and the development of secondary sex characteristics, namely uterine and mammary effects, they also play important roles in almost every physiologic system of the body Edwards, in both women and men Lombardi et al.