Abstract
The G-protein-coupled estrogen receptor-1 (GPER-1), also known as GPR30, is a novel estrogen receptor mediating estrogen receptor signaling in multiple cell types. The progress of estrogen-related cancer is promoted by GPER-1 activation through mitogen-activated protein kinases (MAPK), phosphoinositide 3-kinase (PI3K), and phospholipase C (PLC) signaling pathways. However, this promoting effect of GPER-1 is nonclassic estrogen receptor (ER) dependent manner. In addition, clinical evidences revealed that GPER-1 is associated with estrogen resistance in estrogen-related cancer patients. These give a hint that GPER-1 may be a novel therapeutic target for the estrogen-related cancers. However, preclinical studies also found that GPER-1 activation of its special agonist G-1 inhibits cancer cell proliferation. This review aims to summarize the characteristics and complex functions of GPER-1 in cancers.
Highlights
Estrogen is an important hormone in human beings, especially in females
Majority of the study results addressed that activation of G-protein-coupled estrogen receptor-1 (GPER-1) by estrogen and GPER-1-specific compound 1 (G-1) results in the downstream signals and target genes activation, which promotes the proliferation, migration, and invasion of cancer cells
This effect is in nonclassical Estrogen receptors (ER) expression dependent manner in most cancers except for ovarian cancers
Summary
Estrogen is an important hormone in human beings, especially in females. It plays several important physiological and pathological roles in reproductive system and other systems. Increasing attention has been paid to revealing of the functions of estrogen in physiological and pathological conditions. Estrogen receptors (ER) α and β, the two well established nuclear estrogen receptors, have different physiological functions depending upon their various distributions [1]. The activity of ERβ is opposed to ERα in many systems. Lots of evidences show that estrogen induces the proliferation of cancer cells in breast, uterus, and ovarian cancer through ERα. Increasing studied are focused on the roles of GPER-1 in different types of cancers, the functions of GPER-1 in cancers remain unclear yet. Characteristics and functions of reproductive system cancer will be summarized and discussed in the present review
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