Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors" (PDF). (wikipedia.org)
We performed this meta-analysis to evaluate the efficacy and safety of glucagon-like peptide-1 receptor-agonists (GLP-1RA) treatment on cardio-metabolic parameters among antipsychotic-treated patients with schizophrenia. (frontiersin.org)
It works as a postsynaptic neurotoxin binding to the receptor as an extracellular ligand by interacting with OH group leaving the acetylcholine channel open which releases ions used in creating an action potential. (proteopedia.org)
There must be 5 molecules of cobra toxin (red) to block the receptor (blue) as each molecule binds with an individual alpha chain on the acetylcholine receptor. (proteopedia.org)
The 2nd image depicts an individual toxin binding with one chain on the receptor, both in the same color. (proteopedia.org)
The α-2 adrenergic receptor (A2AR) inhibits insulin or glucagons release. (proteopedia.org)
The human β2 adrenergic receptor bound to a G-protein ( 3sn6 ) is featured in a scene above, and additional structures are on the Adrenergic receptor page . (proteopedia.org)
The human glucagon-like peptide-1 receptor (GLP1R) is shown in gold, cpGFP in green, and residue targets of mutagenesis are shown in magenta. (elifesciences.org)
Hormones are secreted from one cell and bind to a specific receptor on (or in) the target cell. (quizlet.com)
Insulin moves through the blood and binds to receptor proteins located in the membrane of target cells, major ones being liver, skeletal muscle and fat. (quizlet.com)
Glucagon moves through the blood and binds to receptor proteins located in the membrane of liver cells (hepatocytes). (quizlet.com)
Toward this goal, we synthesized an exendin-4 conjugated magnetic iron oxide-based nanoparticle probe targeting glucagon-like peptide 1 receptor (GLP-1R), which is highly expressed on the surface of pancreatic β-cells. (diabetesjournals.org)
K ATP channels are composed of a small inwardly rectifying K + channel subunit (K ir 6.1 or K ir 6.2) plus a sulfonylurea receptor (SUR1, SUR2A or SUR2B) belonging to the ATP-binding cassette superfamily [ 1 ]. (guidetomalariapharmacology.org)
Prearranged positive allosteric modulators (PAMs) inspired by photopharmacology are synthesized and applied to the glucagon-like peptide-1 receptor (GLP-1R), a class B G protein-coupled receptor. (wiley.com)
Considering vitamin D-binding proteins (DBP), which could bind and transport vitamin D to vitamin D receptor (VDR) in the nucleus, was highly present in human islet α-cells and also seen in islet β-cells, 25(OH)D may also contribute to glucagon secretion from α-cells. (researchsquare.com)
Liraglutide is an acylated human Glucagon-Like Peptide-1 (GLP-1) receptor agonist with 97% amino acid sequence homology to endogenous human GLP-1(7-37). (empr.com)
Like GLP-1(7-37), liraglutide activates the GLP-1 receptor, a membrane-bound cell-surface receptor coupled to adenylyl cyclase by the stimulatory G-protein, Gs, in pancreatic beta cells. (empr.com)
understanding the domain structure of the full-length glucagon receptor bound to peptide ligands ( Yang, Yang, 2015 ). (nysbc.org)
Comparative efficacy of 5 sodium glucose cotransporter 2 inhibitor and 7 glucagon-like peptide 1 receptor agonists interventions on cardiorenal outcomes in type 2 diabetes patients: A network meta-analysis based on cardiovascular or renal outcome trials. (omicsdi.org)
Sodium glucose cotransporter 2 (SGLT2) inhibitors and glucagon-like peptide 1 receptor agonists (GLP-1 RAs) have been demonstrated to be able to improve the cardiovascular and renal prognosis in patients with type 2 diabetes (T2D). (omicsdi.org)
To determine unambiguously if suppression of glucagon action will eliminate manifestations of diabetes, we expressed glucagon receptors in livers of glucagon receptor-null (GcgR -/- ) mice before and after β-cell destruction by high-dose streptozotocin. (elsevierpure.com)
Restoration of receptor expression using adenovirus containing the GcgR cDNA restored hepatic GcgR, phospho-cAMP response element binding protein (P-CREB), and phosphoenol pyruvate carboxykinase, markers of glucagon action, rose dramatically and severe hyperglycemia appeared. (elsevierpure.com)
Recent studies also advocate triple agonism with molecules also capable of binding the glucagon receptor. (bvsalud.org)
Although the additive insulinotropic effects of dual glucagon-like peptide-1 receptor (GLP-1R) and glucose-dependent insulinotropic peptide receptor (GIPR) agonism were anticipated based on the known actions of either glucagon-like peptide-1 (GLP-1) or glucose-dependent insulinotropic peptide (GIP) alone, the additional benefits from GCGR were largely unexpected. (bvsalud.org)
Interaction of organochlorine compounds with thyroid receptor, transthyretin, and thyroid-binding globulin. (cdc.gov)
Receptors6
Because the neurobiological substrate of cariprazine has remained elusive, we took advantage of PharmacoSTORM to provide in vivo evidence that cariprazine predominantly binds to D 3 dopamine receptors on Islands of Calleja granule cell axons but avoids dopaminergic terminals. (nature.com)
Semaglutide mimics a hormone called glucagon-like peptide-1 (GLP-1) that binds to GLP-1 receptors. (popsci.com)
Sulfonylureas bind to receptors that are associated with potassium channels sensitive to adenosine triphosphate in beta-cell membrane. (medscape.com)
When glucagon binds to the glucagon receptors, the liver cells convert the storage polysaccharide glycogen into individual glucose molecules and release them into the bloodstream, thereby increasing blood glucose levels. (quizlet.com)
For example, the pancreatic release of insulin in response to glucose is partially mediated by the binding of glucose to sweet-taste receptors on cells of the intestine and subsequent activation of the signaling cascade. (the-scientist.com)
Gut-expressed gustducin and taste receptors regulate secretion of glucagon-like peptide-1," PNAS , 104:15069-74, 2007. (the-scientist.com)
Insulin15
Regarding Type 1 diabetes(T1D), animal/islet-cell studies found that GABA promotes insulin secretion, inhibits α-cell glucagon and dampens immune inflammation, while GAD immunization may also preserve β-cells. (nature.com)
The binding inhibits efflux of potassium ions from the cells, resulting in depolarization, influx of calcium ions, and release of preformed insulin. (medscape.com)
Sulfonylureas may also cause the decrease of serum glucagon and potentiate the action of insulin at the extrapancreatic tissues. (medscape.com)
Pre-treatment of hepatocytes with either glucagon, TPA or insulin did not affect the ability of pertussis toxin to cause the NAD+-dependent, [32P]ADP-ribosylation of alpha-Gi in membrane fractions isolated from such pre-treated hepatocytes. (strath.ac.uk)
Semaglutide stimulates insulin and blocks the release of glucagon "in a glucose-dependent manner," states Novo Nordisk's press release. (diabetesdaily.com)
Islets contain the cells that make hormones, including insulin and glucagon, which keep blood sugar balanced in healthy people. (jax.org)
Insulin-like growth factor binding-protein (IGFBP) -1 concentrations decrease after insulin administration irrespective of meal ingestion. (diva-portal.org)
As for abdominal obesity group, there was the significant association between 25(OH)D and HbA1c, glucagon, HOMA-IR, baseline insulin and C-p. (researchsquare.com)
Glucagon and insulin respectively secreted from the pancreatic islet α-cells and β-cells are main hormones for regulating glucose homeostasis. (researchsquare.com)
Recent studies showed that glucagon served as an insulinotropic hormone rather than counter-regulatory hormone to insulin [ 3 ] , which suggested that both a-and β-cells dysfunction contribute to the development of type 2 diabetes (T2D). (researchsquare.com)
Recently some studies reveal that α-cells lacking DBP secrete less glucagon in response to low glucose concentration despite vitamin D sufficiency[10], and glucagon has a physiologic role to activate β-cells and enhance insulin secretion especially in the fed state [ 11 ] . (researchsquare.com)
Because glucagon acts in functional opposition to insulin in blood glucose homeostasis, blocking glucagon formation and enhancing proinsulin cleavage with a single compound could represent an attractive therapeutic approach in diabetes. (nih.gov)
Recent evidence shows that these SGLT2 inhibitors with low SGLT2/SGLT1 selectivity elevate the level of circulating glucagon like peptide-1 (GLP-1), an incretin hormone that promotes insulin secretion in pancreatic β cells. (omicsdi.org)
Secretion4
Further, GABA-deficient islets did not show appropriate glucagon inhibition in response to increasing glucose concentrations in vitro 22 , suggesting that GABA is directly involved in the suppression of glucagon secretion in pancreatic alpha cells. (nature.com)
So in response to high glucose level or in type 2 diabetes, how 25(OH)D impact glucagon secretion from islet α-cells as well as the islet function homeostasis between islet α-cells and β-cells should be elucidated, which can provide new strategies for treating glucose metabolism disorders. (researchsquare.com)
Liraglutide also decreases glucagon secretion in a glucose-dependent manner. (empr.com)
cells regulates glucagon secretion in mice, possibly explaining the distinct effects of SGLT2 inhibitors on plasma glucagon levels. (omicsdi.org)
But the common factor for many of these changes was its effect on the area where RFX is predicted to bind, in the cells of pancreatic islets. (jax.org)
Proteins2
Normal total serum calcium concentration ranges from 8.8 to 10.4 mg/dL (2.20 to 2.60 mmol/L). About 40% of the total blood calcium is bound to plasma proteins, primarily albumin. (msdmanuals.com)
Cell surface proteins that bind somatostatin and trigger intracellular changes which influence the behavior of cells. (bvsalud.org)
Hepatocytes1
Such actions were mimicked by treatment of hepatocytes with either glucagon or TH-glucagon, an analogue of glucagon which is incapable of activating adenylate cyclase and elevating intracellular cyclic AMP concentrations. (strath.ac.uk)
Hormones3
The Secretin family is a small family of 15 GPCRs (GPCR-B1) that all have an extracellular hormone-binding domain and bind peptide hormones . (axonmedchem.com)
Calcium is also involved in the action of other intracellular messengers, such as cAMP (cyclic adenosine monophosphate) and inositol 1,4,5-triphosphate, and thus mediates the cellular response to numerous hormones, including epinephrine , glucagon , vasopressin (antidiuretic hormone), secretin, and cholecystokinin. (msdmanuals.com)
Serum4
Of the secondary outcomes, the combination GABA/GAD reduced fasting and meal-stimulated serum glucagon, while the safety/tolerability of GABA was confirmed. (nature.com)
This is an area which allows the drug to bind to albumin, which increases its serum half-life and enables weekly dosing while slowing its entry into the bloodstream. (medscape.com)
The Linco Research Glucagon assay utilizes 125 I-labeled Glucagon and a Glucagon antiserum to determine the level of Glucagon in serum, plasma or tissue culture media by the double antibody/PEG technique. (lincoresearch.com)
Anthropometric indices, biochemical parameters, serum 25(OH)D, and islet function including C-peptide (C-p) and glucagon were measured. (researchsquare.com)
Agonists2
Other oral agents besides sulfonylureas are used to treat type 2 diabetes, including biguanides, alpha-glucosidase inhibitors, thiazolidinediones, selective sodium-glucose cotransporter 2 (SGLT2) inhibitors, glucagon-like peptide-1 (GLP-1) agonists, and dipeptidyl peptidase IV (DPP-4) inhibitors. (medscape.com)
The structure has two main regions - one with greater GLP-1 specificity and the other with greater glucagon specificity, and these two areas are linked by a propriety technology called a EuPort ™ domain. (medscape.com)
Inhibitors1
Effect of Sodium Glucose Cotransporter 2 Inhibitors With Low SGLT2/SGLT1 Selectivity on Circulating Glucagon-Like Peptide 1 Levels in Type 2 Diabetes Mellitus. (omicsdi.org)
Albumin1
Semaglutide is intended as a once-weekly type 2 diabetes treatment and is an "investigational analog of native human glucagon-like peptide-1 (GLP-1) and, through its high albumin binding resulting in a long half-life of approximately one week, semaglutide is suitable for once-weekly dosing. (diabetesdaily.com)
Decrease1
Thus, the amount of tracer bound to antibody will decrease as the concentration of unlabeled antigen increases. (lincoresearch.com)
Homeostasis1
Duration of diabetes influence the effect of 25(OH)D on the ratio of glucagon/C-p, on behalf of islet function homeostasis, in T2D patients with abdominal obesity. (researchsquare.com)
Liver1
The Glucagon-Sensitive Adenyl Cyclase System in Plasma Membranes of Rat Liver: II. (nih.gov)
RFX and other factors don't bind directly to the part of a gene that encodes a protein that does a cellular job. (jax.org)
BACKGROUND: Retinol-binding protein 2 (RBP2) is an intracellular carrier for vitamin A in the absorptive enterocytes. (bvsalud.org)
2000. Assessing the role of ortho -substitution on polychlorinated biphenyl binding to transthyretin, a thyroxine transport protein. (cdc.gov)
Diabetes8
They report that many diabetes-linked DNA changes affect the ability of RFX to bind to specific locations in the genomes of pancreas cell clusters called islets. (jax.org)
But when genetic changes linked to Type 2 diabetes are present, that runway gets disrupted, and RFX can't bind as it should. (jax.org)
Each DNA change might alter this binding in a different way, leading to a slightly different effect on Type 2 diabetes risk or blood sugar regulation. (jax.org)
Glucagon-like peptide-1 (GLP-1) and strategies based on this blood sugar-reducing and appetite-suppressing hormone are used to treat obesity and type-2 diabetes. (ku.dk)
The moderate analyses revealed significantly interaction effect of 25(OH)D and glucagon on C-p ( P =0.0124), as well as the effect of 25(OH)D and duration of diabetes on glucagon/C-p in abdominal obesity group. (researchsquare.com)
According to the range of the duration of diabetes, the conditional indirect effect of 25(OH)D on glucagon/C-p was significantly at 1 SD below the mean ( P =0.0002) and the mean of the duration of diabetes ( P =0.0007). (researchsquare.com)
In conclusion, the metabolic manifestations of diabetes cannot occur without glucagon action and, once present, disappear promptlywhen glucagon action is abolished. (elsevierpure.com)
Glucagon suppression should be a major therapeutic goal in diabetes. (elsevierpure.com)
In radioimmunoassay, a fixed concentration of labeled tracer antigen is incubated with a constant dilution of antiserum such that the concentration of antigen binding sites on the antibody is limited, for example, only 50% of the total tracer concentration may be bound by antibody. (lincoresearch.com)
Similar to chronic pharmacological inhibition of DP4, DP4 deficient rats exhibited a phenotype involving reduced diet-induced body weight gain and improved glucose tolerance associated with increased levels of glucagon-like peptide-1 (GLP-1) and bound leptin as well as decreased aminotransferases and triglycerides. (mcw.edu)
Both a high- and a low-fat meal increase the postprandial concentrations of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide 1 (GLP-1) and suppress the postprandial ghrelin levels in adolescents with T1DM. (diva-portal.org)
The OLS regression and quantile regression further showed that 25(OH)D was associated with glucagon and fasting C-p levels in T2D patients with abdominal obesity. (researchsquare.com)
Tissue1
Small molecules readily penetrate tissue preparations and bind their targets with known stoichiometry. (nature.com)
Catalytic1
An X-ray structure of the macrocycle bound to IDE reveals that it engages a binding pocket away from the catalytic site, which explains its remarkable selectivity. (mingsheng88.org)
Response3
The binding of an agonist to them causes a sympathetic response. (proteopedia.org)
a ) Maximal fluorescence response to 10 μM glucagon-like peptide-1 (GLP-1) of the prototype GLP-1 sensor and the N-terminus deletion variants (16 or 23 first amino acids). (elifesciences.org)
a ) Maximal response of GLPLight1 binding pocket variants to 1 μM glucagon-like peptide-1 (GLP-1) (7-37). (elifesciences.org)
Cells2
b ) Representative images showing GLPLight1 expression and fluorescence intensity change before (left) and after (center) addition of 10 μM glucagon-like peptide-1 (GLP-1) (7-37) as well as their respective pixel-wise ΔF/F 0 images in HEK293T cells (top) and primary cortical neurons (bottom). (elifesciences.org)
d ) One-photon excitation/emission spectra of GLPLight1-expressing HEK293T cells before (dark green and dark blue) and after (light green and light blue) addition of 10 μM GLP-1 (7-37) normalized to the peak excitation and emission of the GLP-1-bound state of the sensor. (elifesciences.org)
Distinct1
The co-transcriptional regulatory binding site on the lipins is a conserved LxxIL motif, which is distinct from the active site. (aocs.org)
Sites2
If unlabeled antigen is added to this system, there is competition between labeled tracer and unlabeled antigen for the limited and constant number of binding sites on the antibody. (lincoresearch.com)
In support of kinetic data suggesting that PC2 inhibition probably occurs via an allosteric mechanism, we identified several possible allosteric binding sites using computational searches. (nih.gov)
Level2
With increase in 25(OH)D level, FPG, HbA1c, glucagon and C-p were significantly decreased in trend in T2D patients. (researchsquare.com)
25(OH)D level was associated with HbA1c, glucagon and HOMA-β in non-abdominal obesity group after adjustment. (researchsquare.com)
Specific1
Thus, the four basic necessities for a radioimmunoassay system are: a specific antiserum to the antigen to be measured, the availability of a radioactive labeled form of the antigen, a method whereby antibody-bound tracer can be separated from the unbound tracer, and finally, an instrument to count radioactivity. (lincoresearch.com)
Safety1
The FDA is not bound by the committee's recommendation, but it takes its advice into consideration when reviewing data concerning the safety and efficacy of marketed drugs or new drug applications. (diabetesdaily.com)