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A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins. They are sometimes called blockers; examples include alpha blockers, beta blockers, and calcium channel blockers. In pharmacology, antagonists have affinity but no efficacy for their cognate receptors, and binding will disrupt the interaction and inhibit the function of an agonist or inverse agonist at receptors. Antagonists mediate their effects by binding to the active site or to the allosteric site on a receptor, or they may interact at unique binding sites not normally involved in the biological regulation of the receptor's activity. Antagonist activity may be reversible or irreversible depending on the longevity of the antagonist–receptor complex, which, in turn, depends on the nature of antagonist–receptor binding. The majority of drug antagonists achieve their potency by competing with endogenous ligands or substrates at structurally defined binding sites on receptors.
Anti-obesity medication or weight loss medications are pharmacological agents that reduce or control excess body fat. These medications alter one of the fundamental processes of the human body, weight regulation, by: reducing appetite and consequently energy intake, increasing energy expenditure, redirecting nutrients from adipose to lean tissue, or interfering with the absorption of calories.
Amylin, or islet amyloid polypeptide (IAPP), is a 37-residue peptide hormone. It is co-secreted with insulin from the pancreatic β-cells in the ratio of approximately 100:1 (insulin:amylin). Amylin plays a role in glycemic regulation by slowing gastric emptying and promoting satiety, thereby preventing post-prandial spikes in blood glucose levels.
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Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of drugs that act as antagonists of the calcitonin gene-related peptide receptor (CGRPR).
Deborah Lucy Hay is a New Zealand academic. In 2022, she was elected a Fellow of the Royal Society Te Apārangi.
Dual amylin and calcitonin receptor agonists (DACRAs) are a class of drugs that act as agonists at the amylin receptor and calcitonin receptor that are under development as therapies for obesity and type 2 diabetes. Examples are cagrilintide and the KBP family derived from salmon calcitonin, including KBP‐042, KBP-066A, KBP-089, and KBP-336.
References
- ↑ Hay, D.L.; Christopoulos, G.; Christopoulos, A.; Sexton, P.M. (2004). "Amylin receptors: molecular composition and pharmacology". Biochemical Society Transactions. 32 (5): 865–867. doi:10.1042/BST0320865. PMID 15494035.
- ↑ Cao, Jianjun; Belousoff, Matthew J.; Liang, Yi-Lynn; Johnson, Rachel M.; Josephs, Tracy M.; Fletcher, Madeleine M.; Christopoulos, Arthur; Hay, Debbie L.; Danev, Radostin; Wootten, Denise; Sexton, Patrick M. (25 March 2022). "A structural basis for amylin receptor phenotype". Science. 375 (6587): eabm9609. doi:10.1126/science.abm9609. ISSN 0036-8075. PMID 35324283. S2CID 247677182.
- ↑ Dehestani, Babak; Stratford, Nicholas RS; le Roux, Carel W (30 December 2021). "Amylin as a Future Obesity Treatment". Journal of Obesity & Metabolic Syndrome. 30 (4): 320–325. doi:10.7570/jomes21071. ISSN 2508-6235. PMC 8735818 . PMID 34929674.
- ↑ Bower, Rebekah L; Hay, Debbie L (June 2016). "Amylin structure–function relationships and receptor pharmacology: implications for amylin mimetic drug development". British Journal of Pharmacology. 173 (12): 1883–1898. doi:10.1111/bph.13496. ISSN 0007-1188. PMC 4882495 . PMID 27061187.
- ↑ Garelja, Michael L.; Walker, Christopher S.; Hay, Debbie L. (February 2022). "CGRP receptor antagonists for migraine. Are they also AMY 1 receptor antagonists?". British Journal of Pharmacology. 179 (3): 454–459. doi: 10.1111/bph.15585 . ISSN 0007-1188. PMID 34076887. S2CID 235296644.
- ↑ Hay, Debbie L. (May 2017). "Amylin". Headache: The Journal of Head and Face Pain. 57 (S2): 89–96. doi:10.1111/head.13077. PMID 28485843. S2CID 221752755.
- ↑ Sonne, Nina; Karsdal, Morten A.; Henriksen, Kim (1 April 2021). "Mono and dual agonists of the amylin, calcitonin, and CGRP receptors and their potential in metabolic diseases". Molecular Metabolism. 46: 101109. doi:10.1016/j.molmet.2020.101109. ISSN 2212-8778. PMC 8085567 . PMID 33166741.
- ↑ Fu, Wen; Patel, Aarti; Kimura, Ryoichi; Soudy, Rania; Jhamandas, Jack H. (August 2017). "Amylin Receptor: A Potential Therapeutic Target for Alzheimer's Disease". Trends in Molecular Medicine. 23 (8): 709–720. doi:10.1016/j.molmed.2017.06.003. PMID 28694141.
- ↑ Mietlicki-Baase, Elizabeth G. (1 July 2018). "Amylin in Alzheimer's disease: Pathological peptide or potential treatment?". Neuropharmacology. 136 (Pt B): 287–297. doi:10.1016/j.neuropharm.2017.12.016. ISSN 0028-3908. PMC 5994175 . PMID 29233636.
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