Cardioprotective role of G-Protein Coupled Estrogen Receptor 1 (GPER1).
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.
The University of Iowa, Internal Medicine , Iowa City , USA.
Sivaramakrishna
S
Koganti
D000818:Animals; D002316:Cardiotonic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D002318:Cardiovascular Diseases / Q000188:drug therapy / Q000378:metabolism / Q000517:prevention & control*; D003517:Cyclopentanes / Q000494:pharmacology / Q000627:therapeutic use; D066246:ErbB Receptors / Q000378:metabolism; D005786:Gene Expression Regulation; D006801:Humans; D020782:Matrix Metalloproteinases / Q000378:metabolism; D011804:Quinolines / Q000494:pharmacology / Q000627:therapeutic use; D044140:Receptor, Angiotensin, Type 1 / Q000378:metabolism*; D011960:Receptors, Estrogen / Q000378:metabolism*; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000378:metabolism*
C517943:1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta(c)quinolin-8-yl)ethanone; D002316:Cardiotonic Agents; D003517:Cyclopentanes; C109584:GPER1 protein, human; D011804:Quinolines; D044140:Receptor, Angiotensin, Type 1; D011960:Receptors, Estrogen; D043562:Receptors, G-Protein-Coupled; C512478:EGFR protein, human; D066246:ErbB Receptors; D020782:Matrix Metalloproteinases
Cardiovascular pharmacology; G-protein coupled receptor; hypertension