Amylin receptor

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The amylin receptors (AMYRs) are heterodimers of the calcitonin receptor and receptor activity modifying proteins (RAMPs). They are bound to by amylin with high affinity and consist of AMY1, AMY2, and AMY3. [1] [2] Amylin mimetics that are agonists at the amylin receptors are being developed as therapies for diabetes and obesity, and one, pramlintide, has been FDA approved. [3] [4] The AMY1 receptor may be activated by both amylin and the calcitonin gene-related peptide (CGRP) and could play a role in the effects of CGRP receptor antagonists developed for migraine. [5] [6] Dual agonists of the amylin and calcitonin receptors (DACRAs) are under development for obesity. [7] Amylin and its receptors are believed to play a role in Alzheimer's disease. [8] [9]


References

  1. ↑ 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.
  2. ↑ 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.
  3. ↑ 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.
  4. ↑ 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.
  5. ↑ 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.
  6. ↑ 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.
  7. ↑ 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.
  8. ↑ 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.
  9. ↑ 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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