ArticleBritish journal of pharmacology2006
Regulation of ERK1/2 activity by ghrelin-activated growth hormone secretagogue receptor 1A involves a PLC/PKCvarepsilon pathway.
Article in British journal of pharmacology, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 75 citations in OpenAlex.
- Neuroendocrine crosstalk between sex and metabolic hormones: mechanisms and implications across the female reproductive spectrum.Discover endocrinology and metabolism · 2026Review
- Beyond Hunger: The Structure, Signaling, and Systemic Roles of Ghrelin.International journal of molecular sciences · 2025Review
- Loss-of-Function GHSR Variants Are Associated With Short Stature and Low IGF-I.The Journal of clinical endocrinology and metabolism · 2025Article
- Ghrelin-LEAP2 interactions along the stomach-liver axis.Endocrine journal · 2025Review
- MC4R Variants Modulate α-MSH and Setmelanotide Induced Cellular Signaling at Multiple Levels.The Journal of clinical endocrinology and metabolism · 2024Article
- Insights on discovery, efficacy, safety and clinical applications of ghrelin receptor agonist capromorelin in veterinary medicine.Veterinary research communications · 2024Review
- Identification of the Ghrelin and Cannabinoid CBInternational journal of molecular sciences · 2021Article
- Ghrelin and Cannabinoid Functional Interactions Mediated by Ghrelin/CBFrontiers in cellular neuroscience · 2021Article
- Acylated Ghrelin and The Regulation of Lipid Metabolism in The Intestine.Scientific reports · 2019Article
- Acylated ghrelin prevents doxorubicin-induced cardiac intrinsic cell death and fibrosis in rats by restoring IL-6/JAK2/STAT3 signaling pathway and inhibition of STAT1.Naunyn-Schmiedeberg's archives of pharmacology · 2019Article
- Signal transduction pathways activated by insulin-like peptide 5 at the relaxin family peptide RXFP4 receptor.British journal of pharmacology · 2017Article
- The novel nonapeptide acein targets angiotensin converting enzyme in the brain and induces dopamine release.British journal of pharmacology · 2016Article
- Allomyrina Dichotoma Larvae Regulate Food Intake and Body Weight in High Fat Diet-Induced Obese Mice Through mTOR and Mapk Signaling Pathways.Nutrients · 2016Article
- Agonism, Antagonism, and Inverse Agonism Bias at the Ghrelin Receptor Signaling.The Journal of biological chemistry · 2015Article
- KATP channels in the nodose ganglia mediate the orexigenic actions of ghrelin.The Journal of physiology · 2015Article
- Diet-induced obesity causes peripheral and central ghrelin resistance by promoting inflammation.The Journal of endocrinology · 2015Article
- Article
- G Protein and β-arrestin signaling bias at the ghrelin receptor.The Journal of biological chemistry · 2014Article
- Functionally biased signalling properties of 7TM receptors - opportunities for drug development for the ghrelin receptor.British journal of pharmacology · 2013Review
- Peptide hormone ghrelin enhances neuronal excitability by inhibition of Kv7/KCNQ channels.Nature communications · 2013Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. The growth hormone secretagogue receptor 1a (GHSR-1a) is a G-protein coupled receptor, involved in the biological actions of ghrelin by triggering inositol phosphates and calcium intracellular second messengers. It has also been reported that ghrelin could activate the 44- and 42-kDa extracellular signal-regulated protein kinases (ERK1/2) in different cell lines, but it is not clear whether this regulation is GHSR-1a dependent or not. 2. To provide direct evidence for the coupling of GHSR-1a to ERK1/2 activation, this pathway has been studied in a heterologous expression system. 3. Thus, in Chinese hamster ovary (CHO) cells we showed that ghrelin induced, via the human GHSR-1a, a transient and dose-dependent activation of ERK1/2 leading to activation of the transcriptional factor Elk1. 4. We then investigated the precise mechanisms involved in GHSR-1a-mediated ERK1/2 activation using various specific inhibitors and dominant-negative mutants and found that internalization of GHSR-1a was not necessary. Our results also indicate that phospholipase C (PLC) was involved in GHSR-1a-mediated ERK1/2 activation, however, pathways like tyrosine kinases, including Src, and phosphoinositide 3-kinases were not found to be involved. GHSR-1a-mediated ERK1/2 activation was abolished both by a general protein kinase C (PKC) inhibitor, Gö6983, and by PKC depletion using overnight pretreatment with phorbol ester. Moreover, the calcium chelator, BAPTA-AM, and the inhibitor of conventional PKCs, Gö6976, had no effect on the GHSR-1a-mediated ERK1/2 activation, suggesting the involvement of novel PKC isoforms (epsilon, delta), but not conventional or atypical PKCs. Further analyses suggest that PKCepsilon is required for the activation of ERK1/2. 5. Taken together, these data suggest that ghrelin, through GHSR-1a, activates the Elk1 transcriptional factor and ERK1/2 by a PLC- and PKCepsilon-dependent pathway.
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