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Glucagon-like Peptide 1 Receptor
The glucagon-like peptide-1 receptor (GLP1R) is a G protein-coupled receptor (GPCR) found on beta cells of the pancreas and on neurons of the brain. It is involved in the control of blood sugar level by enhancing insulin secretion. In humans it is synthesised by the gene ''GLP1R'', which is present on chromosome 6. It is a member of the glucagon receptor family of GPCRs. GLP1R is composed of two domains, one extracellular (ECD) that binds the C-terminal helix of GLP-1, and one transmembrane domain (TMD) that binds the N-terminal region of GLP-1. In the TMD domain a fulcrum of polar residues regulates the biased signaling of the receptor while the transmembrane helical boundaries and extracellular surface are a trigger for biased agonism. Ligands GLP1R binds glucagon-like peptide-1 (GLP1) and glucagon as its natural endogenous agonists. Agonists: *GLP-1 – endogenous in humans *glucagon – endogenous in humans *oxyntomodulin * exendin-4, *exenatide * lixisenatide * albigluti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
G Protein-coupled Receptor
G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily related proteins that are cell surface receptors that detect molecules outside the cell and activate cellular responses. They are coupled with G proteins. They pass through the cell membrane seven times in the form of six loops (three extracellular loops interacting with ligand molecules, three intracellular loops interacting with G proteins, an N-terminal extracellular region and a C-terminal intracellular region) of amino acid residues, which is why they are sometimes referred to as seven-transmembrane receptors. Text was copied from this source, which is available under Attribution 2.5 Generic (CC BY 2.5) licence/ref> Ligands can bind either to the extracellular N-terminus and loops (e.g. glutamate receptors) or to the binding site wi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Efpeglenatide
Efpeglenatide is a GLP-1 receptor agonist Glucagon-like peptide-1 (GLP-1) receptor agonists, also known as GLP-1 analogs, GLP-1RAs, or incretin mimetics, are a class of anorectic drugs that reduce blood sugar and energy intake by activating the GLP-1 receptor. They mimic the actions of ... under development for the treatment of type 2 diabetes and obesity and reducing the risk of cardiovascular incidents in people with these conditions. Its developer is Hanmi Pharmaceutical. References GLP-1 receptor agonists Experimental diabetes drugs Peptide therapeutics Amino acids {{gastrointestinal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tirzepatide
Tirzepatide is an antidiabetic medication used to treat type2 diabetes and for weight loss. Tirzepatide is administered via subcutaneous injections (under the skin). In the United States, it is sold under the brand name Mounjaro for diabetes treatment and Zepbound for weight loss and treatment of obstructive sleep apnea. Tirzepatide is a gastric inhibitory polypeptide (GIP) analog and a GLP-1 receptor agonist. The most common side effects include nausea, vomiting, diarrhea, decreased appetite, constipation, upper abdominal discomfort, and abdominal pain. Developed by Eli Lilly and Company, tirzepatide was approved for treatment of diabetes in the US in May 2022, in the European Union in September 2022, in Canada in November 2022, and in Australia in December 2022. The US Food and Drug Administration (FDA) considers it a first-in-class medication. The FDA approved it for weight loss in November 2023. Also in November 2023, the UK Medicines and Healthcare products Regulatory ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ecnoglutide
Ecnoglutide (XW003) is a GLP-1 agonist being developed for the treatment of obesity and type 2 diabetes Type 2 diabetes (T2D), formerly known as adult-onset diabetes, is a form of diabetes mellitus that is characterized by high blood sugar, insulin resistance, and relative lack of insulin. Common symptoms include increased thirst, frequent .... In preclinical trials, "Ecnoglutide showed a favorable potency, pharmacokinetic, and tolerability profile, as well as a simplified manufacturing process" compared to other GLP-1 agonists. A phase 3 trial published in 2025 showed double-digit weightloss over a 48 week treatment. References GLP-1 receptor agonists Experimental diabetes drugs {{Med-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Taspoglutide
Taspoglutide is a former experimental drug, a glucagon-like peptide-1 agonist (GLP-1 agonist), that was under investigation for treatment of type 2 diabetes and being codeveloped by Ipsen and Roche. Initially, phase II trials reported it was effective and well tolerated. Of the eight planned phase III clinical trials of weekly taspoglutide (four against exenatide, sitagliptin, insulin glargine, and pioglitazone), at least five were active in 2009. Preliminary results in early 2010 were favourable. (At least one of the eight planned phase III trials had not started recruiting by end 2009.) In September 2010 Roche halted Phase III clinical trials due to instances of serious hypersensitivity reactions and gastrointestinal side effects. no new trials have been registered since 2010. Chemistry Taspoglutide is the peptide with the sequence His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Aib-Arg-NH2, where Aib is 2-ami ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Semaglutide
Semaglutide is an anti-diabetic medication used for the treatment of type2 diabetes and an anti-obesity medication used for long-term weight management. It is a peptide similar to the hormone glucagon-like peptide-1 (GLP-1), modified with a side chain. It can be administered by subcutaneous injection or taken orally. It is sold by Novo Nordisk under the brand names Ozempic and Rybelsus for diabetes, and under the brand name Wegovy for weight management and weight loss. Semaglutide is a glucagon-like peptide-1 receptor agonist. The most common side effects include nausea, vomiting, diarrhea, abdominal pain, and constipation. It was approved for medical use in the US in 2017. In 2022, it was the 48th most commonly prescribed medication in the United States, with more than 13million prescriptions. Medical uses In the US, semaglutide is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type2 diabetes; and to reduce the risk of major a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
