G protein‐coupled estrogen receptor and estrogen receptor ligands regulate colonic motility and visceral pain

Zielińska, Marta; Fichna, Jakub; Bashashati, Mohammad; Habibi, Salar; Sibaev, Andrei; Timmermans, J.‐P.; Storr, Martin

doi:10.1111/nmo.13025

Cited by 57 publications

(55 citation statements)

References 45 publications

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“…There was a correlation between the expression of GPER in patients with IBS-D and the severity of abdominal pain, and an association between the GPER-mediated estrogenic effects on IBS pathogenesis and activation of mast cells in the colon, thus highlighting a novel avenue for understanding the pathogenesis of sex differences in IBS (77). GPER-mediated estrogenic effects were involved in the regulation of visceral pain and GI motility (78).…”

Section: Estrogen and Estrogen Receptors In Intestinal Diseases Irritmentioning

confidence: 99%

The roles of estrogen and estrogen receptors in gastrointestinal disease (Review)

et al. 2019

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Estrogen is an important sex steroid hormone which serves an important role in the regulation of a number of biological functions, including regulating bone density, brain function, cholesterol mobilization, electrolyte balance, skin physiology, the cardiovascular system, the central nervous system and female reproductive organs. Estrogen exhibits various functions through binding to its specific receptors, estrogen receptor α, estrogen receptor β and G protein-coupled estrogen receptor 1. In recent years, researchers have demonstrated that estrogen and its receptors serve an important role in the gastrointestinal (GI) tract and contribute to the progression of a number of GI diseases, including gastroesophageal reflux, esophageal cancer, peptic ulcers, gastric cancer, inflammatory bowel disease, irritable bowel syndrome and colon cancer. The aim of this review is to provide an overview of estrogen and its receptors in GI disease, and highlight potential avenues for the prevention and treatment of GI diseases.

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Section: Estrogen and Estrogen Receptors In Intestinal Diseases Irritmentioning

confidence: 99%

The roles of estrogen and estrogen receptors in gastrointestinal disease (Review)

et al. 2019

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“…Inflammation would also positively regulate GPER expression, which may add to GPER's neuroprotective effect during postischematic stroke . In addition, GPER activation in the myenteric plexus of the human and rodent colon may lead to decreased colonic motility by promoting NO release from nitrergic nerves …”

Section: What Does Gper Offer To Neuronal Functionmentioning

confidence: 99%

“…In the current issue of Neurogastroenterology and Motility , Zielińska et al. demonstrated that GPER is expressed similarly in the colon and ileum in mice and humans of both genders . The authors also showed both in vitro and in vitro that the GPER agonist (G‐1) inhibited intestinal contractility and significantly prolonged the time to bead expulsion in rats of both genders.…”

Section: Introductionmentioning

confidence: 97%

New roles for neuronal estrogen receptors

Herndon

2017

Neurogastroenterology Motil

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Estrogens encompass steroid hormones which display physiological roles not only in the female reproductive system but also in other organ systems of non-reproductive controls, including the peripheral and central nervous systems. Traditionally, estrogen signals in neurons through a "genomic pathway": binding to estrogen receptors (ERs) which then interact with nuclear estrogen response elements to initiate transcription. This effect is usually delayed at onset (within several hours to days) and prolonged in duration. In addition to these classical ERs, recent data suggest that other ERs function through pregenomic signaling pathways. Estrogen's pregenomic pathways cause intracellular changes within seconds to minutes and go through a novel, 7-transmembrane spanning G protein-coupled receptor (GPER, formerly known as GPR30). In this review, we will briefly cover the cellular and molecular mechanisms of GPER and then discuss newly discovered roles of GPER in cognition, depression, homeostasis, pain processing, and other associated neuronal functions.

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“…ERs are expressed throughout the brain, including the hypothalamus, amygdala, and midbrain, all of which have been shown to send extensive projections to preganglionic vagal neurons of the DMV, and hence modulate GI functions (12,57,63,80). ERs are also expressed on the myenteric plexus of both rodents and humans (1,58,59,90,93).…”

Section: Estrogen Receptor Signaling and Expressionmentioning

confidence: 99%

Role of estrogen and stress on the brain-gut axis

Jiang

Meerveld

Johnson

et al. 2019

American Journal of Physiology-Gastrointestinal and Liver Physi

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Symptoms of functional gastrointestinal disorders (FGIDs), including fullness, bloating, abdominal pain, and altered gastrointestinal (GI) motility, present a significant clinical problem, with a reported prevalence of 25%–40% within the general population. More than 60% of those affected seek and require healthcare, and affected individuals report a significantly decreased quality of life. FGIDs are highly correlated with episodes of acute and chronic stress and are increased in prevalence and reported severity in women compared with men. Although there is evidence that sex and stress interact to exacerbate FGID symptoms, the physiological mechanisms that mediate these sex-dependent disparities are incompletely understood, although hormonal-related differences in GI motility and visceral sensitivity have been purported to play a significant role in the etiology. In this mini review, we will discuss brain-gut axis control of GI motility and sensitivity, the influence of estrogen on GI motility and sensitivity, and stress modulation of the brain-gut axis.

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G protein‐coupled estrogen receptor and estrogen receptor ligands regulate colonic motility and visceral pain

Abstract: GPER and ER receptors are involved in the regulation of GI motility and visceral pain. Both may thus constitute an important pharmacological target in the IBS-D therapy.

Cited by 57 publications

References 45 publications

The roles of estrogen and estrogen receptors in gastrointestinal disease (Review)

The roles of estrogen and estrogen receptors in gastrointestinal disease (Review)

New roles for neuronal estrogen receptors

Role of estrogen and stress on the brain-gut axis

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