G protein-coupled receptor 30 in tumor development
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REVIEW
G protein-coupled receptor 30 in tumor development Dengfeng Wang • Lina Hu • Guonan Zhang Lin Zhang • Chen Chen
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Received: 4 February 2010 / Accepted: 22 June 2010 / Published online: 8 July 2010 Ó Springer Science+Business Media, LLC 2010
Abstract Estrogen plays several important physiological and pathological functions in not only reproductive system but many other systems as well. Its transcriptional activation has been traditionally described as being mediated by classic nuclear estrogen receptors (ERs). It is however established recently that a novel functional estrogen transmembrane receptor, G protein-coupled receptor 30 (GPR30), modulates both rapid non-genomic events and genomic transcriptional events of estrogen. It has been demonstrated that GPR30 promotes the progress of estrogen-related tumors through mitogen-activated protein kinase (MAPK) signaling pathways. Effects mediated by GPR30 are maintained when classic ERs are absent or blocked. In addition, GPR30 is involved in drug resistance, which is often occurring during cancer treatments. All these new findings strongly imply that GPR30 may be an important therapeutic target for estrogen-related tumors. Simultaneously blocking both GPR30 and classic ERs may be a better strategy for the treatment of estrogen-related tumors.
D. Wang G. Zhang Department of Gynecological Oncology, Second People’s Hospital of Sichuan (Sichuan Cancer Hospital), Sichuan 610041, People’s Republic of China D. Wang L. Zhang C. Chen (&) School of Biomedical Sciences, The University of Queensland, Brisbane QLD 4072, Australia e-mail: [email protected] L. Hu Department of Gynecology and Obstetrics, West China Second Hospital, Sichuan University, Sichuan 610041, People’s Republic of China
Keywords Tumor
GPR30 Estrogen receptor Estrogen
Introduction Estrogen is an important hormone in humans, especially in women. It not only contributes to the development and function of female mammary and reproductive system, but also plays a vital role in regulations of skeletal growth and maintenance [1], cardiovascular function [2], central nervous system function [3] and immune reaction [4]. Correspondingly, the disorder of estrogen leads to a number of pathological conditions in above systems, such as endometrial, mammary and skeletal diseases, even tumors. Since its important roles in physiological and pathological conditions of so many systems, estrogen has been an important research topic for several decades. After years of study, the effects of estrogen are believed to be mediated by two wellestablished nuclear estrogen receptors (ERs), ERa and ERb. ERa was firstly described in 1973 [5]; and much later after that, ERb was identified in 1996 [6]. ERa and ERb are encoded by separate genes, ESR1 and ESR2, respectively, but both genes are homologous in the DNA-binding domain (97% amino acid similarity) and ligand-binding domain (60% amino acid similarity) [7]. A clear difference of these two ERs was demonstrated in their tissue distributions [8, 9], which suggested
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