Motilin receptor

Protein-coding gene in the species Homo sapiens

MLNR

Identifiers
Aliases| MLNR, GPR38, MTLR1, motilin receptor
External IDs| OMIM: 602885; HomoloGene: 74398; GeneCards: MLNR; OMA:MLNR - orthologs
| Gene location (Human)

Chr.| Chromosome 13 (human)[1]

Band| 13q14.2| Start| 49,220,338 bp[1]
End| 49,222,377 bp[1]
| RNA expression pattern

Bgee| | Human| Mouse (ortholog)

|

| Top expressed in

* testicle

* gonad

* bone marrow

* fundus

* body of stomach

* islet of Langerhans

* blood

* stromal cell of endometrium

* right lobe of thyroid gland

* kidney

n/a

More reference expression data
BioGPS| |

More reference expression data
| Gene ontology

Molecular function|

* growth hormone-releasing hormone receptor activity
* signal transducer activity
* G protein-coupled receptor activity
* G protein-coupled peptide receptor activity
* hormone binding

Cellular component|

* integral component of membrane
* plasma membrane
* membrane

Biological process|

* G protein-coupled receptor signaling pathway
* signal transduction

Sources:Amigo / QuickGO
| Orthologs

Species| Human| Mouse
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 Mb| n/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

[edit]

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

[edit]

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

[edit]

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.

## Further reading

[edit]

* Smith RG, Leonard R, Bailey AR, Palyha O, Feighner S, Tan C, et al. (February 2001). "Growth hormone secretagogue receptor family members and ligands". Endocrine. 14 (1): 9–14\. doi:10.1385/ENDO:14:1:009. PMID 11322507. S2CID 31807893.
* McKee KK, Tan CP, Palyha OC, Liu J, Feighner SD, Hreniuk DL, et al. (December 1997). "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\. doi:10.1006/geno.1997.5069. PMID 9441746.
* Feighner SD, Tan CP, McKee KK, Palyha OC, Hreniuk DL, Pong SS, et al. (June 1999). "Receptor for motilin identified in the human gastrointestinal system". Science. 284 (5423): 2184–2188\. doi:10.1126/science.284.5423.2184. PMID 10381885.
* Miller P, Roy A, St-Pierre S, Dagenais M, Lapointe R, Poitras P (January 2000). "Motilin receptors in the human antrum". American Journal of Physiology. Gastrointestinal and Liver Physiology. 278 (1): G18 – G23. doi:10.1152/ajpgi.2000.278.1.G18. PMID 10644557. S2CID 41964250.
* Thielemans L, Depoortere I, Van Assche G, Bender E, Peeters TL (March 2001). "Demonstration of a functional motilin receptor in TE671 cells from human cerebellum". Brain Research. 895 (1–2): 119–128\. doi:10.1016/S0006-8993(01)02055-8. PMID 11259768. S2CID 19864565.1–2&rft.pages=119-128&rft.date=2001-03&rft_id=https://api.semanticscholar.org/CorpusID:19864565#id-name=S2CID&rft_id=info:pmid/11259768&rft_id=info:doi/10.1016/S0006-8993(01)02055-8&rft.aulast=Thielemans&rft.aufirst=L&rft.au=Depoortere,+I&rft.au=Van+Assche,+G&rft.au=Bender,+E&rft.au=Peeters,+TL&rfr_id=info:sid/en.wikipedia.org:Motilin+receptor" class="Z3988">
* Coulie B, Matsuura B, Dong M, Hadac EM, Pinon DI, Feighner SD, et al. (September 2001). "Identification of peptide ligand-binding domains within the human motilin receptor using photoaffinity labeling". The Journal of Biological Chemistry. 276 (38): 35518–35522\. doi:10.1074/jbc.M104489200. PMID 11461914.
* Thielemans L, Depoortere I, Vanden Broeck J, Peeters TL (May 2002). "The motilin pharmacophore in CHO cells expressing the human motilin receptor". Biochemical and Biophysical Research Communications. 293 (4): 1223–1227\. doi:10.1016/S0006-291X(02)00356-X. PMID 12054506.
* Depoortere I, Thijs T, Thielemans L, Robberecht P, Peeters TL (May 2003). "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\. doi:10.1124/jpet.102.047563. PMID 12606621. S2CID 2078474.
* Matsuura B, Dong M, Naik S, Miller LJ, Onji M (May 2006). "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\. doi:10.1074/jbc.M511921200. PMID 16531413.

## External links

[edit]

* "Motilin Receptors: Motilin". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2011-05-16. Retrieved 2007-10-25.
* Motilin+receptor at the U.S. National Library of Medicine Medical Subject Headings (MeSH)

* v
* t
* e

Cell surface receptor: G protein-coupled receptors

Class A: Rhodopsin-like

| Neurotransmitter|

| Adrenergic|

* α1 (A
* B
* D)
* α2 (A
* B
* C)
* β1
* β2
* β3

|

Purinergic|

* Adenosine (A1
* A2A
* A2B
* A3)
* P2Y (1
* 2
* 4
* 5
* 6
* 8
* 9
* 10
* 11
* 12
* 13
* 14)

Serotonin|

* (all but 5-HT3) 5-HT1 (A
* B
* D
* E
* F)
* 5-HT2 (A
* B
* C)
* 5-HT (4
* 5A
* 6
* 7)

Other|

* Acetylcholine (M1
* M2
* M3
* M4
* M5)
* Dopamine
* D1
* D2
* D3
* D4
* D5
* GHB receptor
* Histamine
* H1
* H2
* H3
* H4
* Melatonin (1A
* 1B
* 1C)
* TAAR (1
* 2
* 5
* 6
* 8
* 9)

Metabolites and
signaling molecules|

| Eicosanoid|

* CysLT (1
* 2)
* LTB4
* 1
* 2
* FPRL1
* OXE
* Prostaglandin
* DP (1
* 2), EP (1
* 2
* 3
* 4), FP
* Prostacyclin
* Thromboxane

|

Other|

* Bile acid
* Cannabinoid (CB1
* CB2, GPR (18
* 55
* 119))
* EBI2
* Estrogen
* Free fatty acid (1
* 2
* 3
* 4)
* Hydroxycarboxylic acids
* 1
* 2
* 3
* Lysophosphatidic acid (1
* 2
* 3
* 4
* 5
* 6)
* Lysophospholipid (1
* 2
* 3
* 4
* 5
* 6
* 7
* 8)
* Oxoglutarate
* PAF
* Sphingosine-1-phosphate (1
* 2
* 3
* 4
* 5)
* Succinate

Peptide|

| Neuropeptide|

* B/W (1
* 2)
* FF (1
* 2)
* S
* Y (1
* 2
* 4
* 5)
* Neuromedin (B
* U (1
* 2))
* Neurotensin (1
* 2)

|

Other|

* Anaphylatoxin (C3a
* C5a (1
* 2))
* Angiotensin (1
* 2)
* Apelin
* Bombesin
* BRS3
* GRPR
* NMBR)
* Bradykinin (B1
* B2)
* Chemerin
* 1
* 2
* Chemokine
* Cholecystokinin (A
* B)
* Endothelin
* A
* B
* Formyl peptide (1
* 2
* 3)
* FSH
* Galanin (1
* 2
* 3)
* Gonadotropin-releasing hormone (1
* 2)
* Ghrelin
* Kisspeptin
* Luteinizing hormone/choriogonadotropin
* MAS (1
* 1L
* D
* E
* F
* G
* X1
* X2
* X3
* X4)
* Melanocortin (1
* 2
* 3
* 4
* 5)
* MCHR (1
* 2)
* Motilin
* Opioid (Delta
* Kappa
* Mu
* Nociceptin & Zeta, but not Sigma)
* Orexin (1
* 2)
* Oxytocin
* Prokineticin (1
* 2)
* Prolactin-releasing peptide
* Relaxin (1
* 2
* 3
* 4)
* Somatostatin (1
* 2
* 3
* 4
* 5)
* Tachykinin (1
* 2
* 3)
* Thyrotropin
* Thyrotropin-releasing hormone
* Urotensin-II
* Vasopressin (1A
* 1B
* 2)

Miscellaneous|

| Taste, bitter|

* TAS2R
* 1
* 3
* 4
* 5
* 7
* 8
* 9
* 10
* 13
* 14
* 16
* 19
* 20
* 30
* 31
* 38
* 39
* 40
* 41
* 42
* 43
* 45
* 46
* 50
* 60
* Vomeronasal receptor type 1

|

Orphan|

* GPR (3
* 4
* 6
* 12
* 15
* 17
* 18
* 19
* 20
* 21
* 22
* 26
* 27
* 31
* 32
* 33
* 34
* 35
* 37
* 39
* 42
* 45
* 50
* 52
* 55
* 61
* 62
* 63
* 65
* 68
* 75
* 78
* 82
* 83
* 84
* 85
* 87
* 88
* 101
* 103
* 109A
* 109B
* 119
* 120
* 132
* 135
* 137B
* 139
* 141
* 142
* 146
* 148
* 149
* 150
* 151
* 152
* 153
* 160
* 161
* 162
* 171
* 173
* 174
* 176
* 177
* 182
* 183)

Other|

* Adrenomedullin
* Olfactory
* Opsin (3
* 4
* 5
* 1LW
* 1MW
* 1SW
* RGR
* RRH)
* Protease-activated (1
* 2
* 3
* 4)
* SREB (1
* 2
* 3)

Class B: Secretin-like

| Adhesion|

* ADGRB
* Brain-specific angiogenesis inhibitor
* 1
* 2
* 3
* ADGRC
* Cadherin
* 1
* 2
* 3
* ADGRE
* EMR
* 1
* 2
* 3
* CD97
* ADGRG
* 1
* 2
* 3
* 4
* 5
* 6
* 7
* ADGRL
* Latrophilin
* 1
* 2
* 3
* ELTD1

|

Orphan|

* GPR (56
* 64
* 97
* 98
* 110
* 111
* 112
* 113
* 114
* 115
* 116
* 123
* 124
* 125
* 126
* 128
* 133
* 143
* 144
* 155
* 157)

Other|

* Calcitonin
* CALCRL
* Corticotropin-releasing hormone (1
* 2)
* Glucagon (GR
* GIPR
* GLP1R
* GLP2R)
* Growth-hormone-releasing hormone
* PACAPR1
* GPR
* Methuselah-like proteins
* Parathyroid hormone (1
* 2)
* Secretin
* Vasoactive intestinal peptide (1
* 2)

Class C: Metabotropic glutamate / pheromone

| Taste, sweet|

* TAS1R
* 1
* 2
* 3
* Vomeronasal receptor, type 2

|

Other|

* Calcium-sensing receptor
* GABAB (1
* 2)
* Glutamate receptor (Metabotropic glutamate (1
* 2
* 3
* 4
* 5
* 6
* 7
* 8))
* GPRC6A
* GPR (156
* 158
* 179)
* RAIG (1
* 2
* 3
* 4)

Class F: Frizzled & Smoothened

| Frizzled|

* Frizzled (1
* 2
* 3
* 4
* 5
* 6
* 7
* 8
* 9
* 10)

|

Smoothened|

* Smoothened

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