Biology:Motilin receptor

From HandWiki
Short description: Protein-coding gene in the species Homo sapiens


A representation of the 3D structure of the protein myoglobin showing turquoise α-helices.
Generic protein structure example

Motilin receptor is a G protein-coupled receptor (previously GPCR38)[1][2][3] that binds motilin.[4][5] It was first cloned in 1999 by Merck Laboratories.[6] and scientists have since been searching for compounds to modify its behavior.[7]

The primary structure of the motilin receptor consists of 412 amino acids,[6] while its tertiary structure resembles a golf club.[8] The protein C-terminal protein protects from enzymatic degradation, while the N-terminal is essential for binding.[8]

Function

The primary function of the motilin receptor is to contract gastric smooth muscle during phase III of the migrating motor complex (MMC).[6] In this final phase of the MMC, N-type motilin receptors in the distal antral pump of the stomach are activated.[9] This causes contraction of the gastric smooth muscle, sieving food into the small intestine, and priming the stomach for the next meal.[10]

Motilin

Motilin is an intestinal peptide that stimulates the contraction of gastric smooth muscle via the motilin receptor.[6] It is produced by enteroendocrine cells in the proximal small intestine[1][11] and secreted cyclically.[12] Motilin mimetics could be used to increase gastric motility in patients with gastroparesis e.g., constipation-predominant irritable bowel syndrome.[13] However, none of the candidate drugs that have been tested so far have made it to market.[2][14]

References

  1. ↑ 1.0 1.1 "Chapter 7 - Postpyloric Gastrointestinal Peptides" (in en). Physiology of the Gastrointestinal Tract (Fifth ed.). Boston: Academic Press. January 2012. pp. 155–198. doi:10.1016/B978-0-12-382026-6.00007-5. ISBN 978-0-12-382026-6. 
  2. ↑ 2.0 2.1 "Everything you need to know about the motilin receptor" (in en-us). February 2023. https://www.reprocell.com/blog/biopta/motilin-receptor. 
  3. ↑ "The identification of and rationale for drugs which act at the motilin receptor". Progress in Medicinal Chemistry 48: 31–80. 2009. doi:10.1016/s0079-6468(09)04802-4. ISBN 978-0-444-53358-6. PMID 21544957. 
  4. ↑ "Motilin and motilin receptors: characterization and functional significance". Verhandelingen - Koninklijke Academie voor Geneeskunde van Belgie 63 (6): 511–529. 2001. PMID 11813507. 
  5. ↑ "[Evidence for the presence of motilin receptor and a study on the mechanism of motilin induced Ca2+ signaling in rat myenteric neurons]" (in zh). Sichuan da Xue Xue Bao. Yi Xue Ban = Journal of Sichuan University. Medical Science Edition 37 (5): 683–686. September 2006. PMID 17037727. 
  6. ↑ 6.0 6.1 6.2 6.3 "Chapter 170 - Motilin". Handbook of Biologically Active Peptides (Second ed.). San Diego, CA: Academic Press. 2013. pp. 1257–1264. doi:10.1016/B978-0-12-385095-9.00170-6. ISBN 978-0-12-385095-9. 
  7. ↑ "GSK962040: a small molecule motilin receptor agonist which increases gastrointestinal motility in conscious dogs". Neurogastroenterology and Motility 23 (10): 958–e410. October 2011. doi:10.1111/j.1365-2982.2011.01770.x. PMID 21895874. 
  8. ↑ 8.0 8.1 "Chapter 30 - Ghrelin-motilin family" (in en). Handbook of Hormones (Second ed.). San Diego: Academic Press. January 2021. pp. 317–319. doi:10.1016/B978-0-12-820649-2.00082-6. ISBN 978-0-12-820649-2. 
  9. ↑ "Gastrointestinal Motility and Enteric Neuroscience in Health and Disease" (in en). Reference Module in Biomedical Sciences. Elsevier. January 2014. doi:10.1016/B978-0-12-801238-3.00051-9. ISBN 978-0-12-801238-3. 
  10. ↑ "Chapter 152 - Gastrointestinal Hormones and Tumor Syndromes" (in en). Endocrinology (Sixth ed.). Philadelphia: W.B. Saunders. January 2010. pp. 2759–2773. doi:10.1016/B978-1-4160-5583-9.00152-0. ISBN 978-1-4160-5583-9. 
  11. ↑ "Chapter 38 - Gastrointestinal Hormones and Gut Endocrine Tumors" (in en). Williams Textbook of Endocrinology (Thirteenth ed.). Philadelphia: Elsevier. January 2016. pp. 1701–1722. doi:10.1016/B978-0-323-29738-7.00038-1. ISBN 978-0-323-29738-7. 
  12. ↑ "Chapter 7 - Gut Hormones in Pregnancy and Lactation" (in en). Maternal-Fetal and Neonatal Endocrinology. Academic Press. 2020-01-01. pp. 91–99. doi:10.1016/B978-0-12-814823-5.00007-6. ISBN 978-0-12-814823-5. 
  13. ↑ "Sleisenger and Fordtran's Gastrointestinal and Liver Disease: Pathophysiology/Diagnosis/Management—2 Volume Set, 7th Edition" (in en-US). Shock 19 (4): 397–398. April 2003. doi:10.1097/00024382-200304000-00021. ISSN 1540-0514. https://journals.lww.com/shockjournal/Fulltext/2003/04000/Sleisenger_and_Fordtran_s_Gastrointestinal_and.21.aspx. 
  14. ↑ "Pharmacology of Gut Hormone Mimetics for Obesity and Diabetes". Reference Module in Biomedical Sciences. Elsevier. 2022. pp. 301–343. doi:10.1016/B978-0-12-820472-6.00035-9. ISBN 978-0-12-820876-2. https://pure.ulster.ac.uk/en/publications/pharmacology-of-gut-hormone-mimetics-for-obesity-and-diabetes. Retrieved 2023-02-24. 

Further reading

  • "Growth hormone secretagogue receptor family members and ligands". Endocrine 14 (1): 9–14. February 2001. doi:10.1385/ENDO:14:1:009. PMID 11322507. 
  • "Cloning and characterization of two human G protein-coupled receptor genes (GPR38 and GPR39) related to the growth hormone secretagogue and neurotensin receptors". Genomics 46 (3): 426–434. December 1997. doi:10.1006/geno.1997.5069. PMID 9441746. 
  • "Receptor for motilin identified in the human gastrointestinal system". Science 284 (5423): 2184–2188. June 1999. doi:10.1126/science.284.5423.2184. PMID 10381885. 
  • "Motilin receptors in the human antrum". American Journal of Physiology. Gastrointestinal and Liver Physiology 278 (1): G18–G23. January 2000. doi:10.1152/ajpgi.2000.278.1.G18. PMID 10644557. 
  • "Demonstration of a functional motilin receptor in TE671 cells from human cerebellum". Brain Research 895 (1–2): 119–128. March 2001. doi:10.1016/S0006-8993(01)02055-8. PMID 11259768. 
  • "Identification of peptide ligand-binding domains within the human motilin receptor using photoaffinity labeling". The Journal of Biological Chemistry 276 (38): 35518–35522. September 2001. doi:10.1074/jbc.M104489200. PMID 11461914. 
  • "The motilin pharmacophore in CHO cells expressing the human motilin receptor". Biochemical and Biophysical Research Communications 293 (4): 1223–1227. May 2002. doi:10.1016/S0006-291X(02)00356-X. PMID 12054506. 
  • "Interaction of the growth hormone-releasing peptides ghrelin and growth hormone-releasing peptide-6 with the motilin receptor in the rabbit gastric antrum". The Journal of Pharmacology and Experimental Therapeutics 305 (2): 660–667. May 2003. doi:10.1124/jpet.102.047563. PMID 12606621. 
  • "Differential contributions of motilin receptor extracellular domains for peptide and non-peptidyl agonist binding and activity". The Journal of Biological Chemistry 281 (18): 12390–12396. May 2006. doi:10.1074/jbc.M511921200. PMID 16531413. 

External links



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