Prossnitz Eric R, Arterburn Jeffrey B, Smith Harriet O, Oprea Tudor I, Sklar Larry A, Hathaway Helen J
Department of Cell Biology and Physiology, University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA.
Annu Rev Physiol. 2008;70:165-90. doi: 10.1146/annurev.physiol.70.113006.100518.
Steroids play an important role in the regulation of normal physiology and the treatment of disease. Steroid receptors have classically been described as ligand-activated transcription factors mediating long-term genomic effects in hormonally regulated tissues. It is now clear that steroids also mediate rapid signaling events traditionally associated with growth factor receptors and G protein-coupled receptors. Although evidence suggests that the classical steroid receptors are capable of mediating many of these events, more recent discoveries reveal the existence of transmembrane receptors capable of responding to steroids with cellular activation. One such receptor, GPR30, is a member of the G protein-coupled receptor superfamily and mediates estrogen-dependent kinase activation as well as transcriptional responses. In this review, we provide an overview of the evidence for the cellular and physiological actions of GPR30 in estrogen-dependent processes and discuss the relationship of GPR30 with classical estrogen receptors.
类固醇在正常生理调节和疾病治疗中发挥着重要作用。传统上,类固醇受体被描述为配体激活的转录因子,介导激素调节组织中的长期基因组效应。现在很清楚,类固醇还介导传统上与生长因子受体和G蛋白偶联受体相关的快速信号事件。尽管有证据表明经典类固醇受体能够介导许多此类事件,但最近的发现揭示了存在能够通过细胞激活对类固醇作出反应的跨膜受体。一种这样的受体GPR30是G蛋白偶联受体超家族的成员,介导雌激素依赖性激酶激活以及转录反应。在这篇综述中,我们概述了GPR30在雌激素依赖性过程中的细胞和生理作用的证据,并讨论了GPR30与经典雌激素受体的关系。