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The initial product GLP-1 (1–37) is susceptible to amidation and proteolytic cleavage, which gives rise to the two truncated and equipotent biologically active forms, GLP-1 (7–36) amide and GLP-1 (7–37). Active GLP-1 protein secondary structure includes two α-helices from amino acid position 13–20 and 24–35 separated by a linker region.
2740 14652 Ensembl ENSG00000112164 ENSMUSG00000024027 UniProt P43220 O35659 RefSeq (mRNA) NM_002062 NM_021332 RefSeq (protein) NP_002053 NP_067307 Location (UCSC) Chr 6: 39.05 – 39.09 Mb Chr 17: 31.12 – 31.16 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse The glucagon-like peptide-1 receptor (GLP1R) is a G protein-coupled receptor (GPCR) found on beta cells of the pancreas and ...
GLP1 poly-agonist peptides [1] are a class of drugs that activate multiple peptide hormone receptors including the glucagon-like peptide-1 (GLP-1) receptor.These drugs are developed for the same indications as GLP-1 receptor agonists—especially obesity, type 2 diabetes, and non-alcoholic fatty liver disease.
Native GLP-1 is a peptide hormone with a half-life of two minutes because it is rapidly cleared by the enzyme dipeptidyl peptidase-4. [29] As a result, different GLP-1 agonist drugs are modified in various ways to extend the half-life, resulting in drugs that can be dosed multiple times per day, daily, weekly, or less often. [29]
[23] [24] [25] It is a peptide similar to the hormone glucagon-like peptide-1 (GLP-1), modified with a side chain. [ 26 ] [ 27 ] It can be administered by subcutaneous injection or taken orally . [ 14 ] [ 15 ] [ 16 ] [ 28 ] It is sold by Novo Nordisk under the brand names Ozempic [ 14 ] and Rybelsus [ 15 ] for diabetes, and under the brand name ...
Combination GLP-1/glucagon receptor agonists provide the thermogenic benefits of glucagon activation while almost eliminating hyperglycemia induced by glucagon receptor activation. Several such drugs have reached human trials for obesity, diabetes, and non-alcoholic fatty liver disease but adverse effects have hampered development.