Human glucagon receptors receptors glucagon. Medical search. Frequent questions

GLP-1 has multiple effects, including enhancing insulin secretion from pancreatic beta cells in response to glucose, increasing insulin expression, preventing beta-cell apoptosis, promoting the formation of new beta cells, reducing glucagon secretion, slowing down stomach emptying, promoting satiety, and improving glucose disposal in peripheral tissues. (wikipedia.org)
Upon binding to its ligand GLP-1, the GLP-1 receptor activates intracellular signaling pathways that regulate insulin secretion, glucose metabolism, and satiety. (wikipedia.org)
In pancreatic beta cells, GLP-1 receptor activation enhances glucose-stimulated insulin secretion. (wikipedia.org)
GLP-1 receptor signaling in pancreatic alpha cells reduces glucagon secretion, further contributing to glucose lowering. (wikipedia.org)
Glucagon-like peptide 1 (GLP-1) is a gut-derived incretin hormone that stimulates insulin and suppresses glucagon secretion, inhibits gastric emptying, and reduces appetite and food intake. (nih.gov)
The EP3 receptor is stimulated by prostaglandin E2 (PGE2) and couples to G-proteins of the Gi subfamily to decrease intracellular cAMP, blunting glucose-stimulated insulin secretion (GSIS). (nih.gov)
Glucagon concentrations can be elevated in diabetes due to dysregulation of glucagon secretion, while the pancreatic beta-cell can be resistant to the insulinotropic effects of the incretins, both contributing to hyperglycemia. (nih.gov)
Due to the ubiquitous expression of GPCRs throughout various tissues, they are implicated in the regulation of a variety of diverse physiological processes, such as secretion of the blood glucose controlling hormones insulin, glucagon and somatostatin from islets. (bl.uk)
These receptors function in the regulation of numerous physiological processes such as the secretion of insulin, glucagon, and growth hormone, as well as cell growth induced by neuronal excitation in both the central and peripheral nervous system. (atsbio.com)
A physiological feedback system exists between hepatocytes and the alpha cells, termed the liver-alpha cell axis and refers to the relationship between amino acid-stimulated glucagon secretion and glucagon-stimulated amino acid catabolism. (regionh.dk)
Glucagon secretion is also decreased in a glucose-dependent fashion by liraglutide. (creativebiomart.net)
Incubating foreskin fibroblasts with recombinant human SPARC led to increased type I collagen production and decreased matrix metalloproteinase-1 (MMP-1) secretion at the protein and mRNA levels. (bvsalud.org)

GLP1R binds glucagon-like peptide-1 (GLP1) and glucagon as its natural endogenous agonists. (wikipedia.org)
Agonists: GLP-1 - endogenous in humans glucagon - endogenous in humans oxyntomodulin exendin-4, exenatide lixisenatide albiglutide beinaglutide dulaglutide efpeglenatide langlenatide liraglutide semaglutide taspoglutide pegapamodutide lithium chloride Antagonists: [9-39]-GLP-1 T-0632 GLP1R0017 Allosteric modulators Positive: BETP Negative: HTL26119 The GLP-1 receptor is a transmembrane protein composed of seven alpha-helical transmembrane domains (TM1-TM7), an extracellular N-terminus, and an intracellular C-terminus. (wikipedia.org)
Due to these diverse effects, there has been significant interest in developing long-lasting agonists of the GLP-1 receptor (GLP-1R) for the treatment of type 2 diabetes (T2D). (wikipedia.org)
Therapeutic approaches for enhancing incretin action include degradation-resistant GLP-1 receptor agonists (incretin mimetics), and inhibitors of dipeptidyl peptidase-4 (DPP-4) activity (incretin enhancers). (nih.gov)
The most common adverse event associated with GLP-1 receptor agonists is mild nausea, which lessens over time. (nih.gov)
We confirmed that the PGE2-to-EP3 signaling pathway was active in islets from confirmed diabetic BTBR mice and human cadaveric donors, with increased EP3 expression, PGE2 production, and function of EP3 agonists and antagonists to modulate cAMP production and GSIS. (nih.gov)
GLP-1 mimetics are in widespread use to treat diabetes, and a number of glucagon and GIP receptor antagonists and agonists have also been tested as hypoglycemic agents. (nih.gov)
Glucagon-like peptide-1 (GLP-1)-based receptor agonists as a treatment for Parkinson's disease. (nih.gov)
Glucagon-like peptide 1 receptor agonists, peptide drugs that mimic the incretin GLP-1, improve glycemic control among diabetic patients. (asbmb.org)
This year, two papers published in the journal Cell Metabolism reported on trifunctional agonists that can activate all three receptors. (asbmb.org)
In obese mice and monkeys, the triple agonists reduced body weight even in animals that lacked the GLP-1 receptor. (asbmb.org)
The observation that the insulinotropic actions of GLP-1 are reduced in type 2 diabetes mellitus (T2DM) led to the development of incretin-based therapies - GLP-1 receptor agonists and dipeptidyl peptidase 4 (DPP-4) inhibitors - for the treatment of hyperglycaemia in these patients. (nih.gov)
Here, we review the role of GLP-1 and the actions of associated therapies on glucose metabolism, the gut-renal axis, classical renal risk factors, and renal end points in randomized controlled trials of GLP-1 receptor agonists and DPP-4 inhibitors in patients with T2DM. (nih.gov)
Of late, GLP-1 receptor agonists stand apart as a normal treatment for weight decrease and strength. (kobe-jyouryujyo.com)
Hence, individuals taking GLP-1 receptor agonists could experience weight decrease after some time. (kobe-jyouryujyo.com)

Impact of a Weekly Glucagon-Like Peptide 1 Receptor Agonist, Albiglutide, on Glycemic Control and on Reducing Prandial Insulin Use in Type 2 Diabetes Inadequately Controlled on Multiple Insulin Therapy: A Randomized Trial. (medscape.com)
OBJECTIVE: The principle of replacing prandial insulin lispro with a once-weekly glucagon-like peptide 1 receptor agonist (GLP-1RA) for type 2 diabetes inadequately controlled on a multiple daily insulin injections regimen was tested with albiglutide. (medscape.com)
THOUSAND OAKS, Calif. , Dec. 1, 2022 /PRNewswire/ -- Amgen (NASDAQ:AMGN) today announced new Phase 1 data from AMG 133, a novel bispecific glucose-dependent insulinotropic polypeptide receptor (GIPR) antagonist and glucagon-like peptide-1 (GLP-1) receptor agonist molecule. (amgen.com)
AMG 133 is a bispecific glucose-dependent insulinotropic polypeptide receptor (GIPR) antagonist and glucagon-like peptide-1 (GLP-1) receptor agonist molecule. (amgen.com)
Altimmune Inc.'s peptide-based glucagon-like peptide-1/glucagon dual receptor agonist pemvidutide hiccupped in a phase I study earlier this year but has bounced. (bioworld.com)
Further experiments designed to elucidate the target involved in CXCL14 function revealed that CXCL14 is neither an agonist nor an antagonist for the CXCR7 receptor and the putative CXCR4 receptor, and thus these receptors are not responsible for mediating CXCL14 function. (bl.uk)
The first oral form of the glucagon-like peptide-1 receptor agonist, oral semaglutide, has recently been launched and potently controls glycemia and body weight in subjects with type 2 diabetes. (cabi.org)
Sun Pharmaceutical Industries Ltd. announced results from two phase 1 studies evaluating the tolerability, safety, pharmacokinetics and pharmacodynamics of GL0034, a novel long-acting GLP-1 receptor agonist, in non-obese and obese adults without diabetes. (pharmabiz.com)
GL0034 (utreglutide) is an investigational novel glucagon-like peptide 1 receptor agonist (GLP- 1RA) in development as a once-weekly, long-acting, antidiabetic medication in patients with obesity and type 2 diabetes. (pharmabiz.com)
This year, the U.S. Food and Drug Administration approved the first peptide drug that works as a bifunctional agonist of both GLP-1 and GIP receptors. (asbmb.org)
Effects of insulin and the glucagon-like peptide 1 receptor agonist liraglutide on the kidney proteome in db/db mice. (lu.se)
This peptide is a synthetic analog of human glucagon-like peptide-1(GLP-1) and acts as a GLP-1 receptor agonist. (creativebiomart.net)
Liraglutide is an acylated GLP-1 (Glucagon-Like Peptide-1) receptor agonist. (creativebiomart.net)
Kumbar, S. The glucagon-like peptide 1 receptor agonist Exendin-4 induces tenogenesis in human mesenchymal stem cells. (nih.gov)

Effects of skyrin, a receptor-selective glucagon antagonist, in rat and human hepatocytes. (diabetesjournals.org)
On one occasion exendin 9-39, a competitive antagonist of the GLP-1 Receptor (GLP1R), was infused, while on the other saline was infused. (nih.gov)
Here we report the crystal structure of the transmembrane domain of the human corticotropin-releasing factor receptor type 1 in complex with the small-molecule antagonist CP-376395. (nature.com)
L-168,049 is a very potent and selective, non-competitive antagonist of the human glucagon receptor (hGR). (bio-techne.com)

Peptidic glucagon antagonists have been shown to lower blood glucose levels in diabetic models (1-3), but attempts to identify small molecular weight glucagon receptor-binding antagonists have met with little success. (diabetesjournals.org)

Results appeared in the July 25, 2013, issue of Nature along with research from a British group that reported the structure of another class B receptor, corticotropin-releasing factor receptor type 1. (nih.gov)
The corticotropin-releasing factor receptor type 1 is a class B receptor which mediates the response to stress and has been considered a drug target for depression and anxiety. (nature.com)

Peptide hormone receptors overexpressed in human tumors, such as somatostatin receptors, can be used for in vivo targeting for diagnostic and therapeutic purposes. (snmjournals.org)
The somatostatin receptors were the first peptide receptors identified for these purposes, and somatostatin receptor targeting has now become an integral part of the routine management of patients with gastroenteropancreatic neuroendocrine tumors. (snmjournals.org)
Moreover, recent results from clinical studies performing somatostatin receptor radionuclide therapy of these tumors are very promising ( 3 , 4 ). (snmjournals.org)
Prompted by the success of somatostatin receptor targeting, we have evaluated the overexpression of other peptide receptor families in tumors in vitro ( 1 ), with the aim, eventually, of being able to target in vivo a larger spectrum of tumors or individual tumors more efficiently with multiple peptide analogs directed against different peptide receptors expressed in the same tumor ( 5 , 6 ). (snmjournals.org)
Somatostatin Receptor-1 is one of five receptor subtypes termed SSTR1-5. (atsbio.com)
Somatostatin receptors are activated via somatostatin secreted by nerve and endocrine cells. (atsbio.com)
The somatostatin receptor antisera was developed in rabbit using a peptide corresponding to the extracellular domain conjugated to keyhole limpet hemocyanin (KLH) for immunization. (atsbio.com)
Localization of human somatostatin receptor 5 gene (SSTR5) to chromosome band 16p13.3 by fluorescence in situ hybridization. (uchicago.edu)
Human somatostatin receptor genes: localization of SSTR5 to human chromosome 20p11.2. (uchicago.edu)
Human somatostatin receptor genes: localization to human chromosomes 14, 17, and 22 and identification of simple tandem repeat polymorphisms. (uchicago.edu)

The glucagon-like peptide-1 receptor (GLP1R) is a receptor protein found on beta cells of the pancreas and on neurons of the brain. (wikipedia.org)
In humans it is synthesised by the gene GLP1R, which is present on chromosome 6. (wikipedia.org)
Glucagon-like peptide-1 receptor (GLP1R) is a G protein-coupled receptor for the endogenous insulinotropic peptide glucagon-like peptide-1 (GLP-1). (multispaninc.com)

12. Expression and functional activity of glucagon, glucagon-like peptide I, and glucose-dependent insulinotropic peptide receptors in rat pancreatic islet cells. (nih.gov)
Chromosomal assignment and tissue distribution of novel expressed sequence tags from a human pancreatic islet cDNA library. (uchicago.edu)
The gut-derived incretin hormone glucagon-like peptide 1 (GLP-1) is secreted upon meal ingestion and controls glucose metabolism by modulating pancreatic islet cell function, food intake and gastrointestinal motility, amongst other effects. (nih.gov)

Skyrin, a fungal bisanthroquinone, exhibits functional glucagon antagonism by uncoupling the glucagon receptor from adenylate cyclase activation in rat liver membranes (1). (diabetesjournals.org)
2. Cannabinoid receptors CB1 and CB2: a characterization of expression and adenylate cyclase modulation within the immune system. (nih.gov)
8. Effects of delta 9-tetrahydrocannabinol on glucagon receptor coupling to adenylate cyclase in rat liver plasma membranes. (nih.gov)

However, the structures of class B receptors, including the glucagon receptor, have largely remained unsolved because of technical difficulties. (nih.gov)
The structure provides detailed insight into the architecture of class B receptors. (nature.com)

GPCRs are subdivided into classes A, B and C. The structures of several class A receptors have already been uncovered. (nih.gov)
Their work revealed that, typical of GPCRs, the receptor has 7 membrane-spanning sections. (nih.gov)
It differs from class A GPCRs, however, in that it has a wider and deeper pocket for glucagon to bind. (nih.gov)
Structural analysis of class B G-protein-coupled receptors (GPCRs), cell-surface proteins that respond to peptide hormones, has been restricted to the amino-terminal extracellular domain, thus providing little understanding of the membrane-spanning signal transduction domain. (nature.com)
G protein-coupled receptors (GPCRs) are a diverse super family of seven transmembrane spanning proteins whose primary function is to initiate the activation of intracellular signalling pathways following stimulation by extracellular stimuli, which include photons, amines, lipids, ions, peptides and proteins. (bl.uk)
Despite the large array of potential GPCR targets available, only a handful of GPCRs have proven to be successful clinical targets, which may partially be due to the lack of availability of suitable translational models that reflect the human GPCR landscape. (bl.uk)
The aim of the experiments described in this thesis was to compare the mRNA expression profiles of all GPCRs (the GPCRome) and all GPCR peptide ligands (the Secretome) in human and mouse islets in order to determine the suitability of using mouse islets as a translational model for predicting the role of islet GPCRs and GPCR peptide ligands in human islet function. (bl.uk)
Quantitative real-time PCR (qPCR) was used to compare the mRNA expression profiles of 376 GPCRs and 159 GPCR peptide ligands in human islets with their orthologous counterparts in islets isolated from two strains of mice (outbred ICR mice and inbred C57/BL6 mice). (bl.uk)
HGP is modulated by G protein-coupled receptors (GPCRs) and downstream signaling networks. (nih.gov)

It is a member of the glucagon receptor family of G protein-coupled receptors. (wikipedia.org)
It belongs to the class B family of G protein-coupled receptors, also known as secretin-like receptors. (wikipedia.org)
Glucagon works by binding to a G-protein coupled receptor (GPCR). (nih.gov)
The scientists, who have extensive experience working with receptors, used a "fusion protein" to painstakingly create crystals of the glucagon receptor so that the structure could be determined by X-ray crystallography. (nih.gov)
In addition, they altered more than 100 different amino acids in the receptor protein to better understand what parts of the receptor help bind the hormone. (nih.gov)
Glucagon, GLP-1 and GIP are related peptides that target G-protein coupled receptors with effects on glucose and lipid homeostasis. (nih.gov)
Gether, U. Uncovering molecular mechanisms involved in activation of G protein-coupled receptors. (nature.com)
Lagerström, M. C. & Schiöth, H. B. Structural diversity of G protein-coupled receptors and significance for drug discovery. (nature.com)
Molecular signatures of G-protein-coupled receptors. (nature.com)
Rosenbaum, D. M., Rasmussen, S. G. F. & Kobilka, B. K. The structure and function of G-protein-coupled receptors. (nature.com)
NMR structure and peptide hormone binding site of the first extracellular domain of a type B1 G protein-coupled receptor. (nature.com)
Pioszak, A. A. & Xu, H. E. Molecular recognition of parathyroid hormone by its G protein-coupled receptor. (nature.com)
Anatomical profiling of G protein-coupled receptor expression. (guidetopharmacology.org)
15. Co-transfection with protein kinase D confers phorbol-ester-mediated inhibition on glucagon-stimulated cAMP accumulation in COS cells transfected to overexpress glucagon receptors. (nih.gov)
The GLP-1 receptor protein expression was qualitatively and quantitatively investigated in a broad spectrum of human tumors ( n = 419) and nonneoplastic human tissues ( n = 209) with receptor autoradiography using 125 I-GLP-1(7-36)amide. (snmjournals.org)
G protein-coupled peptide hormone receptors play an increasing role in cancer medicine. (snmjournals.org)
Glucagon release counterbalances insulin, preventing hypoglycemia when we eat a high-protein meal. (blogspot.com)
The idea goes like this: glucagon is the opposite of insulin, and if they're released together, as they are when you eat a high-protein meal, then their effects on blood sugar , on hunger , and on fat metabolism cancel one another out in a way that they would not following a carbohydrate-heavy meal. (blogspot.com)
Glucagon does more or less cancel out insulin's effect on blood glucose, and eating protein in isolation does not lead to major changes in blood glucose. (blogspot.com)
But giving humans realistic doses of glucagon, doses that approximate what would occur naturally in the human body following a high-protein meal, does not increase lipolysis ( 5 , 6 ). (blogspot.com)
For example, activation of hepatic glucagon receptors, which are coupled to the stimulatory G protein Gs, leads to a pronounced increase in HGP. (nih.gov)
They are G-protein-coupled receptors characterized by seven transmembrane helices with an extracellular amino terminal domain and an intracellular carboxy terminus. (atsbio.com)
Three-4-month-old female wild type (WT) mice and mice overexpressing human tau and amyloid precursor protein (TAPP) were injected with streptozotocin (STZ) or fed a high-fat diet (HFD). (nih.gov)
Human G-protein-coupled inwardly rectifying potassium channel (GIRK1) gene (KCNJ3): localization to chromosome 2 and identification of a simple tandem repeat polymorphism. (uchicago.edu)
Localization of the gene encoding a neutral amino acid transporter-like protein to human chromosome band 19q13.3 and characterization of a simple sequence repeat DNA polymorphism. (uchicago.edu)
unfolded protein response and endoplasmic reticulum stress - the endoplasmic reticulum is the organelle where complex proteins - including cell membrane receptors - are folded to gain their functional state. (wellnessgarage.ca)

We sought to understand whether 'pancreatic' GLP-1 alters islet function in humans and whether this is affected by type 2 diabetes. (nih.gov)
In analyzing BTBR islet gene expression patterns, we observed that Pgter3, the gene for the prostaglandin E receptor 3 (EP3), was upregulated with diabetes. (nih.gov)
This first-in-human study was designed to evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic effects of AMG 133 in people with obesity and without diabetes (NCT04478708). (amgen.com)
Our results thus indicate that apparently subtoxic neonatal chlorpyrifos exposure, devoid of effects on viability or growth but within the parameters of human fetal or neonatal exposures, produce a metabolic pattern for plasma lipids and insulin that resembles the major adult risk factors for atherosclerosis and type 2 diabetes mellitus. (nih.gov)
The human glucagon-like peptide-1 (GLP-1) receptor is approved in Europe for the treatment of adults with insufficiently controlled type 2 diabetes together with diet and exercise, as monotherapy when metformin is considered inappropriate due to intolerance or contraindications and in addition to other diabetes treatments. (pharmatimes.com)
Type 2 diabetes (T2D) has emerged as one of the major threats to human health in this century. (nih.gov)
Adding glucagon to the mix is expected to have complementary effects on glycemic control, obesity and diabetes. (asbmb.org)

Conversely, when blood glucose levels drop, such as after an overnight fast, the pancreas releases the hormone glucagon, which stimulates liver and muscle cells to release glucose into the bloodstream. (nih.gov)
When researchers put high doses of glucagon on fat cells in a petri dish, or give very high doses of glucagon to animals or humans, it stimulates the release of fat (lipolysis). (blogspot.com)

In the TMD domain there is a fulcrum of polar residues that regulates the biased signaling of the receptor while the transmembrane helical boundaries and extracellular surface are a trigger for biased agonism. (wikipedia.org)
Amgen moved into this Phase 1 study based on human genetic insights and preclinical evidence that suggested synergistic effects with GIP receptor blockade and GLP-1 receptor agonism on weight loss and improvement in other metabolic parameters. (amgen.com)

Atomic details of the interactions of the receptor with the non-peptide ligand that binds deep within the receptor are described. (nature.com)
Binds with high affinity to human GR (IC 50 = 3.7 nM), and moderate affinity to murine and canine GRs (IC 50 values are 63 and 60 nM respectively). (bio-techne.com)

Glucagon helps support blood glucose levels during fasting, when glucose intake is zero, by stimulating the production and release of glucose by the liver. (blogspot.com)
Sun Pharma proceeded into its first-in-human Phase 1 clinical trial based on positive results of its pre-clinical trials in which GL0034 demonstrated robust antidiabetic effects in mice, including reductions in blood glucose levels as well as body weight. (pharmabiz.com)
Moreover, overexpression of barr2 in mouse hepatocytes inhibited glucagon-induced increases of blood glucose levels, further confirming that barr2 acts represents an important negative regulator of hepatic glucagon receptor signaling. (nih.gov)

An experimental gene therapy with the human factor IX gene improved symptoms for as long as 4 years in men with severe hemophilia. (nih.gov)
The structure and function of the human brain is guided by gene expression patterns during prenatal development. (nih.gov)
1993) Human glucagon-like peptide-1 receptor gene: localization to chromosome band 6p21 by fluorescence in situ hybridization and linkage of a highly polymorphic simple tandem repeat DNA polymorphism to other markers on chromosome 6. (multispaninc.com)
Gly40Ser polymorphism of the glucagon receptor gene is associated with central adiposity in men. (cdc.gov)
Sequence of human hexokinase III cDNA and assignment of the human hexokinase III gene (HK3) to chromosome band 5q35.2 by fluorescence in situ hybridization. (uchicago.edu)
Localization of the genes encoding two transcription factors, LMX1 and CDX3, regulating insulin gene expression to human chromosomes 1 and 13. (uchicago.edu)
Localization of the glucagon receptor gene to human chromosome band 17q25. (uchicago.edu)
Human hexokinase II: localization of the polymorphic gene to chromosome 2. (uchicago.edu)
Human glucagon-like peptide-1 receptor gene. (uchicago.edu)
Assignment of the gene encoding glycogen synthase (GYS) to human chromosome 19, band q13.3. (uchicago.edu)
Human hexokinase II gene: exon-intron organization, mutation screening in NIDDM, and its relationship to muscle hexokinase activity. (uchicago.edu)
Human fructose-1,6-bisphosphatase gene (FBP1): exon-intron organization, localization to chromosome bands 9q22.2-q22.3, and mutation screening in subjects with fructose-1,6-bisphosphatase deficiency. (uchicago.edu)

D) Reagents and assays for the accurate expression and quantitation of functional incretin receptors in the endocrine/exocrine cells of the pancreas and relevant extrapancreatic tissues. (nih.gov)
1. Expression of functional glucagon receptors on lymphoid cells. (nih.gov)
10. Functional expression of the rat glucagon-like peptide-I receptor, evidence for coupling to both adenylyl cyclase and phospholipase-C. (nih.gov)
11. Functional expression of the P2Y14 receptor in murine T-lymphocytes. (nih.gov)
However, as assessed by cAMP accumulation assay, only one of the studied cell lines expressed functional CTR, while the other cell lines have functional CGRP (CLR/RAMP1) receptors. (monash.edu)
Exome sequencing data failed to account for the discrepancy between functional data and expression on the cell lines that do not respond to calcitonin(s) with no deleterious non-synonymous polymorphisms detected, suggesting that other factors may be at play, such as alternative splicing or rapid constitutive receptor internalisation. (monash.edu)
1 μ M). In functional studies, inhibits glucagon-stimulated cAMP synthesis in CHO cells expressing hGR (IC 50 = 41 nM), and in murine liver membranes. (bio-techne.com)
1993) Cloning and functional expression of the human glucagon-like peptide-1 (GLP-1) receptor. (multispaninc.com)

GLP-1 receptors were expressed in various endocrine tumors, with particularly high amounts in pheochromocytomas, as well as in brain tumors and embryonic tumors but not in carcinomas or lymphomas. (snmjournals.org)
The gastrointestinal tract - the largest endocrine network in human physiology - orchestrates signals from the external environment to maintain neural and hormonal control of homeostasis. (nih.gov)

Oral semaglutide under human protocols and doses regulates food intake, body weight, and glycemia in diet-induced obese mice. (cabi.org)
Hep-barr2-KO mice showed impaired glucose tolerance, associated with enhanced signaling through hepatic glucagon receptors in vivo and in vitro. (nih.gov)
One particular probable purpose is the fact that Ndfip1 deficiency causes GI pathology that manifests itself differently amongst mice and humans. (glucagon-receptor.com)
Nevertheless, it's clear that Ndfip1 prevents GI illness in mice and may well also avoid the improvement of GI illnesses in humans. (glucagon-receptor.com)
Insulin deficiency, but not resistance, exaggerates cognitive deficits in transgenic mice expressing human amyloid and tau proteins. (nih.gov)

The N-terminus of the receptor is responsible for binding glucagon-like peptide-1 (GLP-1) ligands, while the intracellular C-terminus interacts with intracellular signaling proteins to initiate downstream signaling pathways. (wikipedia.org)
20. Effects of putative cannabinoid receptor ligands, anandamide and 2-arachidonyl-glycerol, on immune function in B6C3F1 mouse splenocytes. (nih.gov)
A Comparison of the Genotoxic Effects of Gold Nanoparticles Functionalized with Seven Different Ligands in Cultured Human Hepatocellular Carcinoma Cells. (ilexlife.com)

5. Expression and signal transduction of the glucagon receptor in betaTC3 cells. (nih.gov)

16. Localization of the domains involved in ligand binding and activation of the glucose-dependent insulinotropic polypeptide receptor. (nih.gov)
In the process of quantifying the GPCR peptide ligand mRNA expression profiles, it was revealed that the orphan chemokine CXCL14 is expressed by both mouse and human islets. (bl.uk)
In summary, the experiments described in this thesis reveal that human and mouse islets exhibit some degree of similarity in GPCR and GPCR peptide ligand mRNA expression, but the suitability of using mouse islets as surrogates for predicting human islet physiology is receptor/receptor family specific. (bl.uk)

Moreover, knowledge of the distribution and putative functions of a peptide receptor in normal tissues is important to estimate the potential of side effects of a peptide therapy ( 10 ). (snmjournals.org)

The GLP-1 receptors may represent a novel molecular target for in vivo scintigraphy and targeted radiotherapy for a variety of GLP-1 receptor-expressing tumors. (snmjournals.org)
To estimate the suitability of a peptide receptor for in vivo tumor targeting, one needs detailed in vitro data on its expression in human tumors and human normal tissues. (snmjournals.org)
One critical prerequisite for successful in vivo targeting is a high receptor expression in tumors, allowing a high tumoral radiotracer accumulation ( 4 , 7 ). (snmjournals.org)
A new promising candidate for in vivo tumor targeting is the GLP-1 receptor, a member of the glucagon receptor family ( 11 ). (snmjournals.org)
Glucagon has a potent effect in isolated fat cells in the laboratory, but appears not to affect fat mobilization in humans in vivo . (blogspot.com)

Measurement of the extracellular acidification rate in CHO cells transfected with the human secretin receptor. (guidetopharmacology.org)
Human Cardiac Progenitor Cell-Derived Extracellular Vesicles Exhibit Promising Potential for Supporting Cardiac Repair in Vitro . (ilexlife.com)

Antigen: Purified recombinant fragment of human GTF2B expressed in E. coli. (glucagon-receptor.com)

These outcomes and sex selectivity resemble earlier findings at the cellular level, which identified hepatic hyperresponsiveness to gluconeogenic inputs from beta-adrenoceptors or glucagon receptors. (nih.gov)
The primary outcome measure will be differences in the glucagon sensitivity index between individuals with and without hepatic steatosis. (regionh.dk)

The objective was to develop an experimental test to determine glucagon sensitivity with respect to amino acid and glucose metabolism in humans. (regionh.dk)

Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. (multispaninc.com)
This antibody was raised against rat somatosatin receptor-1 (SSTR1) and recognizes SSTR1 in human. (atsbio.com)

Another important function of the GLP-1 receptor is the regulation of gastric emptying. (wikipedia.org)
Gastric Emptying: GLP-1 receptor activation slows down the rate at which the stomach empties its contents into the small intestine. (wikipedia.org)

By inhibiting glucagon release, GLP-1 receptor activation helps to maintain glucose homeostasis. (wikipedia.org)
Activation of the receptor delays the rate at which the stomach empties, leading to increased satiety and reduced food intake. (wikipedia.org)
Activation of the GLP-1 receptor promotes feelings of satiety, leading to a reduction in food intake and improved weight management. (wikipedia.org)
We also analyzed the impact of EP3 receptor activation on signaling through the glucagon-like peptide (GLP)-1 receptor. (nih.gov)
The only CTR-expressing cell line (SB2b) showed modest coupling to the cAMP pathway and no activation of other known CTR signaling pathways, including ERK 1/2 and p38 MAP kinases, and Ca 2+ mobilization, supportive of low cell surface receptor expression. (monash.edu)
In the brain, receptor activation elicits neurotrophic actions through protection against metabolic and oxidative insults. (multispaninc.com)

Results: In this study we tested expression and performed pharmacological characterization of the calcitonin receptor (CTR) as well as other members of the calcitonin family of receptors in high-grade glioma (HGG) cell lines derived from individual patient tumours, cultured in defined conditions. (monash.edu)

Anticipating a major development of GLP-1 receptor targeting in nuclear medicine, our aim was to evaluate in vitro the GLP-1 receptor expression in a large variety of other tumors and to compare it with that in nonneoplastic tissues. (snmjournals.org)
For GLP-1 receptor scintigraphy, a low-background signal can be expected, on the basis of the low receptor expression in the normal tissues surrounding tumors. (snmjournals.org)
Equally important is a low receptor expression in normal tissues surrounding tumors, at sites of tumor origin and of metastasis, for receptor-targeted scintigraphy will detect tumors with adequate sensitivity only in the case of a high ratio of tumor to background signal ( 8 , 9 ). (snmjournals.org)
We found a significant increase in miR-1-3p expression in cecal ligation and puncture (CLP) rats exosomes sequencing and sepsis patients' exosomes, and lipopolysaccharide (LPS)-stimulated human umbilical vein endothelial cells (HUVECs) in vitro . (portlandpress.com)

We have examined the effects of skyrin on cells transfected with the human glucagon receptor and on isolated rat and human hepatocytes. (diabetesjournals.org)
In rat hepatocytes, skyrin (30 micromol/l) inhibited glucagon-stimulated cAMP production (53%) and glucose output (IC50 56 micromol/l). (diabetesjournals.org)

14. Effects of targeted deletion of cannabinoid receptors CB1 and CB2 on immune competence and sensitivity to immune modulation by Delta9-tetrahydrocannabinol. (nih.gov)
The proposed glucagon sensitivity test (comprising two elements: 1) i.v. injection of 0.2 mg glucagon and 2) infusion of mixed amino acids 331 mg/hour/kg) is based on nine pilot studies which are presented. (regionh.dk)
Calculation of a proposed glucagon sensitivity index with respect to amino acid catabolism is also described. (regionh.dk)
Secondly, we describe a complete study protocol (GLUSENTIC) according to which the glucagon sensitivity test will be applied in a cross-sectional study currently taking place. (regionh.dk)
Developing a glucagon sensitivity test and index may provide insight into the physiological and pathophysiological mechanism of glucagon action and glucagon-based therapies. (regionh.dk)

NIEHS research uses state-of-the-art science and technology to investigate the interplay between environmental exposures, human biology, genetics, and common diseases to help prevent disease and improve human health. (nih.gov)

Measurement of cAMP levels in CHO cells transfected with the secretin receptor. (guidetopharmacology.org)
This role is based primarily on the peptide receptor overexpression on tumor cells, which allows specific receptor-targeted scintigraphic tumor imaging and tumor therapy with radiolabeled peptide analogs ( 1 ). (snmjournals.org)
thick line: receptor-expressing cells. (multispaninc.com)
Furthermore, lack of significantly advertised bacterial invasion and proliferation in human being epithelial Caco-2 cells and murine macrophages, as well as a notably increasing invasion but not cell-to-cell spread in the murine fibroblasts L929 cells. (bioentryplus.com)
When blood sugar drops, pancreatic alpha cells release glucagon which then triggers the release of glucose from the liver. (wellnessgarage.ca)
Both insulin and glucagon are small proteins recognized by specific receptors on individual cells. (wellnessgarage.ca)
Resveratrol-Elicited PKC Inhibition Counteracts NOX-Mediated Endothelial to Mesenchymal Transition in Human Retinal Endothelial Cells Exposed to High Glucose. (ilexlife.com)

Glucagon-like peptide-1 (GLP-1) is a hormone consisting of 30 amino acids. (wikipedia.org)
Its amino acid sequence, based on GIP, is engineered to bind both GIP and GLP-1 receptors, with modifications to boost its half-life by reducing its susceptibility to proteases and improving its binding to albumin. (asbmb.org)

They then built a structural model of the receptor with glucagon bound to it in order to predict how the hormone and receptor interact. (nih.gov)
The team is now working to determine the exact structure of the receptor when glucagon is bound to it. (nih.gov)
Structure of the human smoothened receptor bound to an antitumour agent. (nature.com)
Two accompanying papers detailed the structure of the GLP-1 receptor when bound by small molecules that affect the receptor's activity. (nih.gov)

Anatomy2

Chemicals and Drugs9

Phenomena and Processes1

Secretion12

Agonists15

Agonist14

Antagonist4

Antagonists1

Corticotropin-releasing factor rec2

Somatostatin10

GLP1R3

Pancreatic islet3

Adenylate cyclase3

Class B receptors2

GPCRs9

Protein26

Diabetes7

Stimulates2

Agonism2

Binds2

Blood glucose levels3

Gene12

Functional8

Endocrine2

Mice5

Ligands3

Signal transduction1

Ligand3

Putative1

Vivo5

Extracellular2

Recombinant1

Hepatic2

Glucose metabolism1

Antibody2

Gastric2

Activation6

Characterization1

Expression4

Hepatocytes2

Sensitivity5

Genetics1

Cells7

Amino2

Bound4