Glucagon: difference between revisions
Diff·revision 13 → 14·04:23, 26 Feb 2025
Difference between revision 13 and revision 14 of Glucagon. 5 lines changed; the page grew by 841 bytes.
| Revision 13 — 08:30, 29 Jan 2025 CuriousCallum (talk) expand §Receptor and signalling 4,913 bytes ±0 | Revision 14 — 04:23, 26 Feb 2025 TirzTaxonomist (talk) the half-life in the lead was the terminal figure; label it as such 5,754 bytes +841 | ||
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| 36 | The receptor relatedness is what makes multi-receptor agonism chemically tractable, and it also makes selectivity a design constraint rather than a given: an unmodified glucagon analogue has appreciable activity at the GLP-1 receptor and vice versa. Reported potency ratios for the multi-receptor peptides are assay-dependent and should be compared only within a single publication's system.{{r|coskun2022}} | 36 | The receptor relatedness is what makes multi-receptor agonism chemically tractable, and it also makes selectivity a design constraint rather than a given: an unmodified glucagon analogue has appreciable activity at the GLP-1 receptor and vice versa. Reported potency ratios for the multi-receptor peptides are assay-dependent and should be compared only within a single publication's system.{{r|coskun2022}} |
| 37 | 37 | ||
| + | 38 | == Therapeutic use as an agonist target == | |
| + | 39 | Chronic glucagon-receptor agonism increases resting energy expenditure by an amount that is modest in absolute terms — figures in the region of 3–8% appear in early-phase work — and increases hepatic fatty-acid oxidation, reducing liver fat. Both are desirable in obesity and in metabolic liver disease.{{r|coskun2022}} | |
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| + | 41 | The obstacle is that the same agonism raises blood glucose. The design solution is a fixed intramolecular ratio: [[Retatrutide|retatrutide]] engages GIP, GLP-1 and glucagon receptors; [[Survodutide|survodutide]] engages glucagon and GLP-1 receptors; efinopegdutide engages glucagon and GLP-1 receptors with a different balance and has been studied principally for hepatic fat. In each case the GLP-1 component is dosed sufficiently to dominate the net glycaemic effect. | |
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| 38 | == References == | 43 | == References == |
| 39 | {{reflist}} | 44 | {{reflist}} |