Amylin receptor

The amylin receptors (AMYRs) are heterodimers of the calcitonin receptor that 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

^ 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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[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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