G-Protein Coupled Estrogen Receptor 1 (GPER1), also known as G-Protein Coupled Receptor 30 (GPR30) and initially considered an orphan receptor, has become one of the most important pharmacological targets in cardiovascular research. Since the gene encoding this putative receptor was cloned nearly 20 years ago, researchers have addressed its role in various aspects of physiology, including cardioprotection. Although extensive research has been carried out to understand the role of GPER1 as a pharmacological target to treat cardiovascular diseases, there are few current reviews addressing the overall cardioprotective benefits of this receptor and the signaling intermediates involved. This review considers the origins of GPER1, its cell biology, its physiological and pharmacological roles as a therapeutic target in cardiovascular disease, and what future research on GPER1 might entail. More specifically, the review focuses on GPER1 regulation of Angiotensin Type I Receptor (AT1R) and the role of estrogen receptors, epidermal growth factor receptor (EGFR) and matrix metalloproteinases (MMPs) in bringing about the cardioprotective effects of GPER1. Areas where improved knowledge of GPER1 biology is still needed to better understand the receptor’s cardioprotective effects are also discussed.

G蛋白偶联雌激素受体1（GPER1），也称为G蛋白偶联受体30（GPR30），最初被认为是孤儿受体，已成为心血管研究中最重要的药理靶标之一。自从大约20年前克隆了编码这种推定受体的基因以来，研究人员已经研究了其在生理学各个方面的作用，包括心脏保护作用。尽管已经进行了广泛的研究以了解GPER1作为治疗心血管疾病的药理学靶标的作用，但是目前很少有针对该受体和涉及的信号传导中间体的整体心脏保护作用的综述。这篇评论考虑了GPER1的起源，细胞生物学，作为心血管疾病治疗靶点的生理和药理作用，以及将来可能对GPER1进行的研究。更具体地说，本综述着重于血管紧张素I型受体（AT1R）的GPER1调节以及雌激素受体，表皮生长因子受体（EGFR）和基质金属蛋白酶（MMP）在实现GPER1的心脏保护作用中的作用。还讨论了仍需要提高GPER1生物学知识以更好地了解受体的心脏保护作用的领域。