G-1

GPR30 is a transmembrane G protein-coupled receptor (GPCR) localized to endoplasmic reticulum (ER) that binds estradiol with high affinity, activating multiple intracellular signaling pathways.¹ G-1 is a nonsteroidal, high-affinity, selective agonist of GPR30 that binds with a K_i value of 11 nM. Competitive binding studies in estrogen receptor α- (ERα-) and ERβ-expressing cells yielded K_i values for estradiol of 0.30 and 0.38 nM, respectively, with no substantial binding of G-1 at 1 µM.² The discovery of G-1, a compound that does not bind classical ERs, should facilitate further physiological experiments to define the role of GPR30 in vivo.

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1. Revankar, C.M., Cimino, D.F., Sklar, L.A., et al. A transmembrane intracellular estrogen receptor mediates rapid cell signaling. Science 307(5715), 1625-1630 (2005).

2. Bologa, C.G., Revankar, C.M., Young, S.M., et al. Virtual and biomolecular screening converge on a selective agonist for GPR30. Nat. Chem. Biol. 2(4), 207-212 (2006).

Yang, Y., Wang, Y., Zou, H., et al. GPER1 signaling restricts macrophage proliferation and accumulation in human hepatocellular carcinoma. Front. Immunol. 15, 10.3389/fimmu.2024.1481972 (2024).