Amylin receptor agonist (revision 2)
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| Amylin receptor agonist | |
|---|---|
| Endogenous ligand | Amylin |
| Receptors | AMY1, AMY2, AMY3 (calcitonin receptor plus RAMP) |
| Design problem | Removing amyloidogenicity from the human sequence |
| Topic infobox · conventions | |
Amylin receptor agonists are engineered analogues of amylin designed to reproduce its actions on gastric emptying, glucagon secretion and food intake without the aggregation behaviour of the native human sequence.[1]
Two generations exist. Pramlintide, approved in 2005 as an adjunct to insulin, substitutes three prolines into the human sequence to disrupt β-sheet formation; its short half-life requires injection at each meal, which limited uptake. Cagrilintide is a long-acting analogue employing acylation for weekly dosing and is under development principally in combination with semaglutide as CagriSema.[2]
References
- ^ Hay DL, Chen S, Lutz TA, Parkes DG, Roth JD. "Amylin: pharmacology, physiology, and clinical potential." Pharmacological Reviews 67(3):564–600 (2015). PMID 26071095.
- ^ Lau DCW, Erichsen L, Francisco AM, et al. "Once-weekly cagrilintide for weight management in people with overweight and obesity: a multicentre, randomised, double-blind, placebo-controlled trial." The Lancet 398(10317):2160–2172 (2021). PMID 34798060.
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