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Motilin receptor

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From Wikipedia, the free encyclopedia

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	49,220,338bp^[1]
Band	13q14.2	End	49,222,377bp^[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 aG protein-coupled receptor (previously GPCR38)^[3]^[4]^[5] that bindsmotilin.^[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]

Theprimary structure of the motilin receptor consists of 412 amino acids,^[8] while itstertiary structure resembles a golf club.^[10] The proteinC-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 gastricsmooth muscle during phase III of themigrating 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 intestinalpeptide 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 increasegastric motility in patients withgastroparesis e.g., constipation-predominantirritable bowel syndrome.^[15] However, none of the candidate drugs that have been tested so far have made it to market.^[4]^[16]

References

[edit]

^^a ^b ^cGRCh38: Ensembl release 89: ENSG00000102539 –Ensembl, May 2017
^"Human PubMed Reference:".National Center for Biotechnology Information, U.S. National Library of Medicine.
^^a ^bGomez 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.
^^a ^bPuckrin Z (February 2023)."Everything you need to know about the motilin receptor".www.reprocell.com. Retrieved2023-02-24.
^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.
^Depoortere I (2001). "Motilin and motilin receptors: characterization and functional significance".Verhandelingen - Koninklijke Academie voor Geneeskunde van Belgie.63 (6):511–529.PMID 11813507.
^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.
^^a ^b ^c ^dPoitras 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.
^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.
^^a ^bKaiya 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.
^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.
^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.
^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.
^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.
^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.
^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. Retrieved2023-02-24.

External links

[edit]

"Motilin Receptors: Motilin".IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived fromthe original on 2011-05-16. Retrieved2007-10-25.
Motilin+receptor at the U.S. National Library of MedicineMedical Subject Headings (MeSH)

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 but5-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)
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 notSigma)
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 (1 3 4 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 78 81 82 83 84 85 87 88 92 101 103 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 GABA_B (1 2) Glutamate receptor (Metabotropic glutamate (1 2 3 4 5 6 7 8)) GPRC6A GPR (156 158 179) RAIG (1 2 3 4)