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Motilin receptor

MLNR
Identifiers
AliasesMLNR, GPR38, MTLR1, motilin receptor
External IDsOMIM: 602885; HomoloGene: 74398; GeneCards: MLNR; OMA:MLNR - orthologs
Orthologs
SpeciesHumanMouse
Entrez

2862

n/a

Ensembl

ENSG00000102539

n/a

UniProt

O43193

n/a

RefSeq (mRNA)

NM_001507

n/a

RefSeq (protein)

NP_001498

n/a

Location (UCSC)Chr 13: 49.22 – 49.22 Mbn/a
PubMed search[2]n/a
Wikidata
View/Edit Human

Motilin receptor is a G protein-coupled receptor (previously GPCR38)[3][4][5] that binds motilin.[6][7] It was first cloned in 1999 by Merck Laboratories.[8] and scientists have since been searching for compounds to modify its behavior.[9]

The primary structure of the motilin receptor consists of 412 amino acids,[8] while its tertiary structure resembles a golf club.[10] The protein C-terminal protein protects from enzymatic degradation, while the N-terminal is essential for binding.[10]

Function

The primary function of the motilin receptor is to contract gastric smooth muscle during phase III of the migrating motor complex (MMC).[8] In this final phase of the MMC, N-type motilin receptors in the distal antral pump of the stomach are activated.[11] This causes contraction of the gastric smooth muscle, sieving food into the small intestine, and priming the stomach for the next meal.[12]

Motilin

Motilin is an intestinal peptide that stimulates the contraction of gastric smooth muscle via the motilin receptor.[8] It is produced by enteroendocrine cells in the proximal small intestine[3][13] and secreted cyclically.[14] Motilin mimetics could be used to increase gastric motility in patients with gastroparesis e.g., constipation-predominant irritable bowel syndrome.[15] However, none of the candidate drugs that have been tested so far have made it to market.[4][16]

References

  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000102539 – Ensembl, May 2017
  2. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  3. ^ a b Gomez GA, Englander EW, Greeley GH (January 2012). "Chapter 7 - Postpyloric Gastrointestinal Peptides". In Johnson LR, Ghishan FK, Kaunitz JD, Merchant JL (eds.). Physiology of the Gastrointestinal Tract (Fifth ed.). Boston: Academic Press. pp. 155–198. doi:10.1016/B978-0-12-382026-6.00007-5. ISBN 978-0-12-382026-6.
  4. ^ a b Puckrin Z (February 2023). "Everything you need to know about the motilin receptor". www.reprocell.com. Retrieved 2023-02-24.
  5. ^ Westaway SM, Sanger GJ (2009). "The identification of and rationale for drugs which act at the motilin receptor". Progress in Medicinal Chemistry. 48: 31–80. doi:10.1016/s0079-6468(09)04802-4. ISBN 978-0-444-53358-6. PMID 21544957.
  6. ^ Depoortere I (2001). "Motilin and motilin receptors: characterization and functional significance". Verhandelingen - Koninklijke Academie voor Geneeskunde van Belgie. 63 (6): 511–529. PMID 11813507.
  7. ^ Yang X, Dong L, Yang H (September 2006). "[Evidence for the presence of motilin receptor and a study on the mechanism of motilin induced Ca2+ signaling in rat myenteric neurons]". Sichuan da Xue Xue Bao. Yi Xue Ban = Journal of Sichuan University. Medical Science Edition (in Chinese). 37 (5): 683–686. PMID 17037727.
  8. ^ a b c d Poitras P (2013). "Chapter 170 - Motilin". Handbook of Biologically Active Peptides (Second ed.). San Diego, CA: Academic Press. pp. 1257–1264. doi:10.1016/B978-0-12-385095-9.00170-6. ISBN 978-0-12-385095-9.
  9. ^ Leming S, Broad J, Cozens SJ, Otterson M, Winchester W, Lee K, et al. (October 2011). "GSK962040: a small molecule motilin receptor agonist which increases gastrointestinal motility in conscious dogs". Neurogastroenterology and Motility. 23 (10): 958–e410. doi:10.1111/j.1365-2982.2011.01770.x. PMID 21895874. S2CID 21813655.
  10. ^ a b Kaiya H (January 2021). "Chapter 30 - Ghrelin-motilin family". In Ando H, Ukena K, Nagata S (eds.). Handbook of Hormones (Second ed.). San Diego: Academic Press. pp. 317–319. doi:10.1016/B978-0-12-820649-2.00082-6. ISBN 978-0-12-820649-2. S2CID 242138545.
  11. ^ Surjanhata BC, Kuo B (January 2014). "Gastrointestinal Motility and Enteric Neuroscience in Health and Disease". Reference Module in Biomedical Sciences. Elsevier. doi:10.1016/B978-0-12-801238-3.00051-9. ISBN 978-0-12-801238-3.
  12. ^ Taheri S, Ghatei MA, Bloom SR (January 2010). "Chapter 152 - Gastrointestinal Hormones and Tumor Syndromes". In Jameson JL, De Groot LJ (eds.). Endocrinology (Sixth ed.). Philadelphia: W.B. Saunders. pp. 2759–2773. doi:10.1016/B978-1-4160-5583-9.00152-0. ISBN 978-1-4160-5583-9.
  13. ^ Vella A (January 2016). "Chapter 38 - Gastrointestinal Hormones and Gut Endocrine Tumors". In Melmed S, Polonsky KS, Larsen PR, Kronenberg HM (eds.). Williams Textbook of Endocrinology (Thirteenth ed.). Philadelphia: Elsevier. pp. 1701–1722. doi:10.1016/B978-0-323-29738-7.00038-1. ISBN 978-0-323-29738-7.
  14. ^ Shim J, Yu R (2020-01-01). "Chapter 7 - Gut Hormones in Pregnancy and Lactation". In Kovacs CS, Deal CL (eds.). Maternal-Fetal and Neonatal Endocrinology. Academic Press. pp. 91–99. doi:10.1016/B978-0-12-814823-5.00007-6. ISBN 978-0-12-814823-5. S2CID 208557201.
  15. ^ de Villiers WJ (April 2003). "Sleisenger and Fordtran's Gastrointestinal and Liver Disease: Pathophysiology/Diagnosis/Management—2 Volume Set, 7th Edition". Shock. 19 (4): 397–398. doi:10.1097/00024382-200304000-00021. ISSN 1540-0514.
  16. ^ Lafferty R, O'Harte F, Irwin N, Flatt PR, Gault VA (2022). "Pharmacology of Gut Hormone Mimetics for Obesity and Diabetes". Reference Module in Biomedical Sciences. Elsevier. pp. 301–343. doi:10.1016/B978-0-12-820472-6.00035-9. ISBN 978-0-12-820876-2. S2CID 234190503. Retrieved 2023-02-24.

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