Estrogen (GPER) Receptors

The GPER (G protein-coupled estrogen receptor, GPR30) is a membrane protein that binds estrogen leading to estrogen-mediated adenylyl cyclase stimulation. The receptor is widely distributed in neural, breast, placental, heart, ovarian, prostate and hepatic tissues.

Products
Background
Pathways (1)
Gene Data

Estrogen (GPER) Receptor Agonists

Cat. No. Product Name / Activity
7811 CITFA
Potent G protein-coupled estrogen receptor (GPER) agonist
2824 β-Estradiol
Endogenous ER agonist
3577 G-1
Potent and selective GPER agonist
1110 Genistein
GPER agonist. Also tyrosine kinase inhibitor
1047 ICI 182,780
High affinity GPER agonist
1125 Quercetin
GPER agonist. Also non-selective PI 3-kinase inhibitor
0999 Tamoxifen citrate
High affinity GPER agonist

Estrogen (GPER) Receptor Antagonists

Cat. No. Product Name / Activity
6116 BHPI
ERα antagonist; also activates unfolded protein response; active in vivo
7812 CIMBA hydrochloride
Potent and selective G protein-coupled estrogen receptor (GPER) antagonist
3678 G-15
High affinity and selective GPER antagonist
4759 G-36
Selective GPER antagonist

The GPER (G protein-coupled estrogen receptor, GPR30) is a membrane protein that binds estrogen leading to estrogen-mediated adenylyl cyclase stimulation. The receptor is widely distributed in neural, breast, placental, heart, ovarian, prostate, hepatic, vascular epithelial and lymphoid tissues. The GPER binds estradiol with high affinity, but has lower affinity for the other estrogens, estrone and estriol. The receptor acts independently of ERα and ERβ and triggers ER-dependent EGFR action.

External sources of pharmacological information for Estrogen (GPER) Receptors :

Pathways for Estrogen (GPER) Receptors

Estrogen Signaling Pathway

Estrogen Signaling Pathway

Estrogen is a steroid hormone that is responsible for the regulation of growth, differentiation and function of the reproductive system. Estrogen signaling is often dysregulated in breast cancer and osteoporosis.

Estrogen (GPER) Receptor Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human GPER NM_001039966 Q99527
Mouse Gper NM_029771 Q8BMP4
Rat Gper NM_133573 O08878