雌激素及其相关分子的作用在两性中都是复杂的和多方面的。许多天然、合成和治疗性分子靶向产生和响应于雌激素的通路。多种受体促进这些反应，包括核激素受体家族的经典雌激素受体（雌激素受体α和β），其主要作用是配体激活的转录因子，以及7个跨膜G蛋白偶联的雌激素受体（GPER），它能够激活各种不同的信号通路。 GPER在生理和疾病中的药理学和功能角色揭示了在许多生理系统中对天然和合成雌激素化合物的反应中具有重要作用。这些功能对于治疗包括癌症、心血管疾病和代谢失调在内的许多疾病状态都具有重要意义。本综述着重探讨了GPER的复杂药理学，并总结了GPER的主要生理功能以及GPER靶向化合物的治疗意义和正在进行的应用。

The actions of estrogens and related estrogenic molecules are complex and multifaceted in both sexes. A wide array of natural, synthetic, and therapeutic molecules target pathways that produce and respond to estrogens. Multiple receptors promulgate these responses, including the classical estrogen receptors of the nuclear hormone receptor family (estrogen receptors α and β), which function largely as ligand-activated transcription factors, and the 7-transmembrane G protein-coupled estrogen receptor, GPER, which activates a diverse array of signaling pathways. The pharmacology and functional roles of GPER in physiology and disease reveal important roles in responses to both natural and synthetic estrogenic compounds in numerous physiological systems. These functions have implications in the treatment of myriad disease states, including cancer, cardiovascular diseases, and metabolic disorders. This review focuses on the complex pharmacology of GPER and summarizes major physiological functions of GPER and the therapeutic implications and ongoing applications of GPER-targeted compounds.