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1: Science. 2005 Mar 11;307(5715):1625-30. Epub 2005 Feb 10.Click here to read Links
Comment in:
Science. 2005 Mar 11;307(5715):1572-3.
Science. 2005 Oct 7;310(5745):51-3; author reply 51-3.

A transmembrane intracellular estrogen receptor mediates rapid cell signaling.

Revankar CM, Cimino DF, Sklar LA, Arterburn JB, Prossnitz ER.

Department of Cell Biology and Physiology, University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA.

The steroid hormone estrogen regulates many functionally unrelated processes in numerous tissues. Although it is traditionally thought to control transcriptional activation through the classical nuclear estrogen receptors, it also initiates many rapid nongenomic signaling events. We found that of all G protein-coupled receptors characterized to date, GPR30 is uniquely localized to the endoplasmic reticulum, where it specifically binds estrogen and fluorescent estrogen derivatives. Activating GPR30 by estrogen resulted in intracellular calcium mobilization and synthesis of phosphatidylinositol 3,4,5-trisphosphate in the nucleus. Thus, GPR30 represents an intracellular transmembrane estrogen receptor that may contribute to normal estrogen physiology as well as pathophysiology.

PMID: 15705806 [PubMed - indexed for MEDLINE]

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