GLP-1R
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GLP-1R
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 ...
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Exenatide
Exenatide, sold under the brand name Byetta among others, is a medication used to treat type 2 diabetes. It is used together with diet, exercise, and potentially other antidiabetic medication. It is a treatment option after metformin and sulfonylureas. It is given by injection under the skin. Common side effects include low blood sugar, nausea, dizziness, abdominal pain, and pain at the site of injection. Other serious side effects may include medullary thyroid cancer, angioedema, pancreatitis, and kidney injury. Use in pregnancy and breastfeeding is of unclear safety. Exenatide is a glucagon-like peptide-1 receptor agonist (GLP-1 receptor agonist) also known as incretin mimetics. It works by increasing insulin release from the pancreas and decreases excessive glucagon release. Exenatide was approved for medical use in the United States in 2005. In 2019, it was the 312th most commonly prescribed medication in the United States, with more than 1million prescriptions. ...
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Dulaglutide
Dulaglutide, sold under the brand name Trulicity among others, is a medication used for the treatment of type 2 diabetes in combination with diet and exercise. It is also approved in the United States for the reduction of major adverse cardiovascular events in adults with type 2 diabetes who have established cardiovascular disease or multiple cardiovascular risk factors. The most common side effects are nausea, diarrhea, vomiting, abdominal pain, and decreased appetite. It is a glucagon-like peptide-1 receptor agonist (GLP-1 agonist) consisting of GLP-1(7-37) covalently linked to an Fc fragment of human IgG4. GLP-1 is a hormone that is involved in normalizing the level of glucose in blood (glycemia). The Food and Drug Administration (FDA) approved dulaglutide for use in the United States in September 2014. It was approved for use in the European Union in November 2014. In 2022, it was the 74th most commonly prescribed medication in the United States, with more than 8million ...
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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 ...
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Lixisenatide
Lixisenatide (trade name Lyxumia in the European Union and Adlyxin in the U.S. and manufactured by Sanofi) is a once-daily injectable GLP-1 receptor agonist for the treatment of type 2 diabetes. Medical use Lixisenatide is used as adjunct to diet and exercise to treat type 2 diabetes. In the European Union, its use is limited to complementing insulin therapy. As of 2017 it is unclear if they affect a person's risk of death. It is provided in an autoinjector containing fourteen doses and is injected subcutaneously. Lixisenatide should not be used for people who have problems with stomach emptying. Lixisenatide delays emptying of the stomach, which may change how quickly other drugs that are taken by mouth take effect. Lixisenatide in neurodegenerative diseases Results from a research work which was done by McClean PL et al. demonstrated that the GLP-1 receptor agonists liraglutide and lixisenatide which are on the market as treatments for type 2 diabetes show promise as poten ...
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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 ...
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