Glucagon-like peptide-1: difference between revisions
Diff·revision 26 → 27·01:06, 24 Oct 2024
Difference between revision 26 and revision 27 of Glucagon-like peptide-1. 2 lines changed; the page grew by 443 bytes.
| Revision 26 — 17:34, 18 Oct 2024 EmptyingElke (talk) move table to the section it supports 7,399 bytes +178 | Revision 27 — 01:06, 24 Oct 2024 GastroparesisGwen (talk) add category 7,842 bytes +443 | ||
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| 49 | GLP-1 is cleaved between residues 8 and 9 by [[Dipeptidyl peptidase-4|dipeptidyl peptidase-4]], a widely expressed serine exopeptidase present both as a membrane protein on endothelium and as a soluble plasma form. The resulting GLP-1 (9–36) amide is at best weakly active at the [[GLP-1 receptor]] and has historically been regarded as an inactive metabolite, although a degree of independent cardiovascular activity has been proposed.{{r|deacon1995}} | 49 | GLP-1 is cleaved between residues 8 and 9 by [[Dipeptidyl peptidase-4|dipeptidyl peptidase-4]], a widely expressed serine exopeptidase present both as a membrane protein on endothelium and as a soluble plasma form. The resulting GLP-1 (9–36) amide is at best weakly active at the [[GLP-1 receptor]] and has historically been regarded as an inactive metabolite, although a degree of independent cardiovascular activity has been proposed.{{r|deacon1995}} |
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| + | 51 | The consequence is a plasma half-life of approximately 1.5–2 minutes, and an estimated 50–75% of newly secreted GLP-1 is degraded before it leaves the intestinal capillary bed. Two therapeutic strategies follow directly from this: inhibit the enzyme, which is the mechanism of the gliptin class, or engineer the peptide so that it resists the enzyme, which is the mechanism of the [[GLP-1 receptor agonist|agonist class]].{{r|nauck2018}} | |
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| 51 | == References == | 53 | == References == |
| 52 | {{reflist}} | 54 | {{reflist}} |