The ins and outs of GPR30: A transmembrane estrogen receptor
Estrogen is an important hormone in human physiology. It acts both via transcriptional regulation as well as via modulation of intracellular signaling through second messengers. Although estrogen's transcriptional effects occur through classical nuclear steroid receptors (ERs), recent studies r...
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| Veröffentlicht in: | Journal of steroid biochemistry and molecular biology 2008-04, Vol.109 (3), p.350-353 |
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| container_end_page | 353 |
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| container_issue | 3 |
| container_start_page | 350 |
| container_title | Journal of steroid biochemistry and molecular biology |
| container_volume | 109 |
| creator | Prossnitz, Eric R. Oprea, Tudor I. Sklar, Larry A. Arterburn, Jeffrey B. |
| description | Estrogen is an important hormone in human physiology. It acts both via transcriptional regulation as well as via modulation of intracellular signaling through second messengers. Although estrogen's transcriptional effects occur through classical nuclear steroid receptors (ERs), recent studies reveal the existence of a novel 7-transmembrane G protein-coupled receptor, GPR30, which responds to estrogen and tamoxifen stimulation with rapid cellular signaling including ERK activation, PI3K activation, calcium mobilization and cAMP production. To distinguish between ER- and GPR30-mediated signaling, we have identified a novel GPR30 agonist that exhibits high specificity for GPR30. In this review, we will describe recent work to further our understanding of the role of GPR30 in estrogen biology. |
| doi_str_mv | 10.1016/j.jsbmb.2008.03.006 |
| format | Article |
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It acts both via transcriptional regulation as well as via modulation of intracellular signaling through second messengers. Although estrogen's transcriptional effects occur through classical nuclear steroid receptors (ERs), recent studies reveal the existence of a novel 7-transmembrane G protein-coupled receptor, GPR30, which responds to estrogen and tamoxifen stimulation with rapid cellular signaling including ERK activation, PI3K activation, calcium mobilization and cAMP production. To distinguish between ER- and GPR30-mediated signaling, we have identified a novel GPR30 agonist that exhibits high specificity for GPR30. 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Prostaglandin receptors</subject><subject>Humans</subject><subject>Ligands</subject><subject>Molecular and cellular biology</subject><subject>Protein Binding</subject><subject>Receptors, Estrogen - metabolism</subject><subject>Receptors, G-Protein-Coupled - metabolism</subject><subject>Signaling</subject><issn>0960-0760</issn><issn>1879-1220</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2008</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEFv1DAQhS1ERZfCL0BCvtBbwjh2bAcBUlW1BakSCJWzZTuT1qskXuxspf57vOyqwKWnOcyb9958hLxhUDNg8v26Xmc3uboB0DXwGkA-IyumVVexpoHnZAWdhAqUhGPyMuc1AHDO1AtyzLQAKYGvyMebO6RhztTOPY3bJdM40KvvPzh8oGd0SXbOE06uTKSYlxRvcaYJPW6WmF6Ro8GOGV8f5gn5eXlxc_6luv529fX87LrybcuXSmiHUrJWaufbxjltRasU-H7woGWrWqdAoRi0bn2vRN9zQDX0nXCswa6z_IR83vtutm7C3uNcio1mk8Jk04OJNpj_N3O4M7fx3jRCl1heDE4PBin-2pY_zBSyx3Esb8VtNiVfKq2hCPle6FPMOeHwGMLA7KibtflD3eyoG-CmUC9Xb__t9_fmgLkI3h0ENns7DgWnD_lR14CQIMTO6NNeh4XmfcBksg84e-xDYb6YPoYni_wGsG6g0g</recordid><startdate>20080401</startdate><enddate>20080401</enddate><creator>Prossnitz, Eric R.</creator><creator>Oprea, Tudor I.</creator><creator>Sklar, Larry A.</creator><creator>Arterburn, Jeffrey B.</creator><general>Elsevier Ltd</general><general>Elsevier Science</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>20080401</creationdate><title>The ins and outs of GPR30: A transmembrane estrogen receptor</title><author>Prossnitz, Eric R. ; Oprea, Tudor I. ; Sklar, Larry A. ; Arterburn, Jeffrey B.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c553t-48be661568bc52bb8a45770cdfc086575b707e4f885cd74dd30e7fd94b12e99a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2008</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cell Membrane - metabolism</topic><topic>Cell receptors</topic><topic>Cell structures and functions</topic><topic>Estrogen</topic><topic>Estrogen receptor</topic><topic>Estrogens - metabolism</topic><topic>Fundamental and applied biological sciences. 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| ispartof | Journal of steroid biochemistry and molecular biology, 2008-04, Vol.109 (3), p.350-353 |
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| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Biological and medical sciences Cell Membrane - metabolism Cell receptors Cell structures and functions Estrogen Estrogen receptor Estrogens - metabolism Fundamental and applied biological sciences. Psychology GPR30 Hormone receptors. Growth factor receptors. Cytokine receptors. Prostaglandin receptors Humans Ligands Molecular and cellular biology Protein Binding Receptors, Estrogen - metabolism Receptors, G-Protein-Coupled - metabolism Signaling |
| title | The ins and outs of GPR30: A transmembrane estrogen receptor |
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