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AM833 Is a Novel Agonist of Calcitonin Family G Protein–Coupled Receptors: Pharmacological Comparison with Six Selective and Nonselective Agonists by Madeleine M. Fletcher; Peter Keov; Tin T. Truong; Grace Mennen; Caroline A. Hick; Peishen Zhao; Sebastian G.B. Furness; Thomas Kruse; Trine R. Clausen; Denise Wootten; Patrick M. Sexton is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is AM833 Is a Novel Agonist of Calcitonin Family G Protein–Coupled Receptors: Pharmacological Comparison with Six Selective and Nonselective Agonists about?
Obesity and associated comorbidities are a major health burden, and novel therapeutics to help treat obesity are urgently needed. There is increasing evidence that targeting the amylin receptors (AMYRs), heterodimers of the calcitonin G protein-coupled receptor (CTR) and receptor activity-modifying proteins, improves weight control and has the potential to act additively with other treatments such as glucagon-like peptide-1 receptor agonists. Recent data indicate that AMYR agonists, which can also independently activate the CTR, may have improved efficacy for treating obesity, even though selective activation of CTRs is not efficacious. AM833 (cagrilintide) is a novel lipidated amylin analog that is undergoing clinical trials as a nonselective AMYR and CTR agonist. In the current study, we have investigated the pharmacology of AM833 across 25 endpoints and compared this peptide with AMYR selective and nonselective lipidated analogs (AM1213 and AM1784), and the clinically used peptide agonists pramlintide (AMYR selective) and salmon CT (nonselective). We also profiled human CT and rat amylin as prototypical selective agonists of CTR and AMYRs, respectively. Our results demonstrate t
Who reads AM833 Is a Novel Agonist of Calcitonin Family G Protein–Coupled Receptors: Pharmacological Comparison with Six Selective and Nonselective Agonists?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Madeleine M. Fletcher; Peter Keov; Tin T. Truong; Grace Mennen; Caroline A. Hick; Peishen Zhao; Sebastian G.B. Furness; Thomas Kruse; Trine R. Clausen; Denise Wootten; Patrick M. Sexton
- Publisher
- American Society for Pharmacology & Experimental Therapeutics (ASPET)
- Published
- 2021
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)