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Holecistokininski receptor A
	; PDB prikaz baziran na 1d6g.
Dostupne strukture
	1d6g
Identifikatori
Simboli	CCKAR; CCK-A; CCK1-R; CCKRA
Vanjski ID	OMIM: 118444 MGI: 99478 HomoloGene: 37337 IUPHAR: CCK1 GeneCards: CCKAR Gene
Ontologija gena
Molekularna funkcija	• aktivnost rodopsinu-sličnog receptora; • receptorska aktivnost; • aktivnost holecistokininskog receptora;
Celularna komponenta	• ćelijska membrana; • integralno sa ćelijskom membranom;
Biološki proces	• neuronska migracija; • kontrakcija glatkih mišića; • prenos signala; • G-proteinska signalizacija, spregnuta sa IP3 sekundarnim glasnikom (aktivacija fosfolipaze C); • elevacija citosolne koncentracije jona kalcijuma; • aksonogeneza; • respons na nutrijente; • varenje; • način ishrane; • razvoj prednjeg mozga;
Pregled RNK izražavanja
	podaci
Ortolozi

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Holecistokininski receptor A, CCKAR ili CCK₁, je humani protein. Oznaka CCK₁ je preporučena od strane IUPHAR.

Ovaj gen kodira G-protein spregnuti receptor koji vezuje ne-sulfatisane članove holecistokininske (CCK) familije peptidnih hormona. Ovaj receptor je fiziološki medijator pankreasne enzimske sekrecije i kontrakcije glatkih mišića žučne kese i stomaka. U centralnom i perifernom nervnom sistemu ovaj receptor reguliše zasićenost i oslobađanje beta-endorfina i dopamina.^[1]

Selektivni ligandi

Agonisti

Holecistokinin
CCK-4
SR-146,131
A-71623 - modifikovani tetrapeptid, potentan i selektivan CCK_A agonist, IC₅₀ 3.7nM, 1200x selektivnist u odnosu na CCK_B.

Antagonisti

Proglumid
Lorglumid
Devazepid
Deksloksiglumid
Asperlicin
SR-27897
IQM-95333
JNJ-17156516

Povezano

Reference

↑ „Entrez Gene: CCKAR cholecystokinin A receptor”.

Literatura

Varga G, Bálint A, Burghardt B, D'Amato M (2004). „Involvement of endogenous CCK and CCK1 receptors in colonic motor function.”. Br. J. Pharmacol. 141 (8): 1275–84. DOI:10.1038/sj.bjp.0705769. PMC 1574909. PMID 15100163.
Miller LJ, Holicky EL, Ulrich CD, Wieben ED (1995). „Abnormal processing of the human cholecystokinin receptor gene in association with gallstones and obesity.”. Gastroenterology 109 (4): 1375–80. DOI:10.1016/0016-5085(95)90601-0. PMID 7557108.
Huppi K, Siwarski D, Pisegna JR, Wank S (1995). „Chromosomal localization of the gastric and brain receptors for cholecystokinin (CCKAR and CCKBR) in human and mouse.”. Genomics 25 (3): 727–9. DOI:10.1016/0888-7543(95)80018-H. PMID 7759110.
de Weerth A, Pisegna JR, Huppi K, Wank SA (1993). „Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor.”. Biochem. Biophys. Res. Commun. 194 (2): 811–8. DOI:10.1006/bbrc.1993.1894. PMID 8343165.
Ulrich CD, Ferber I, Holicky E, et al. (1993). „Molecular cloning and functional expression of the human gallbladder cholecystokinin A receptor.”. Biochem. Biophys. Res. Commun. 193 (1): 204–11. DOI:10.1006/bbrc.1993.1610. PMID 8503909.
Kennedy K, Gigoux V, Escrieut C, et al. (1997). „Identification of two amino acids of the human cholecystokinin-A receptor that interact with the N-terminal moiety of cholecystokinin.”. J. Biol. Chem. 272 (5): 2920–6. DOI:10.1074/jbc.272.5.2920. PMID 9006937.
Inoue H, Iannotti CA, Welling CM, et al. (1997). „Human cholecystokinin type A receptor gene: cytogenetic localization, physical mapping, and identification of two missense variants in patients with obesity and non-insulin-dependent diabetes mellitus (NIDDM).”. Genomics 42 (2): 331–5. DOI:10.1006/geno.1997.4749. PMID 9192855.
Gigoux V, Escrieut C, Silvente-Poirot S, et al. (1998). „Met-195 of the cholecystokinin-A receptor interacts with the sulfated tyrosine of cholecystokinin and is crucial for receptor transition to high affinity state.”. J. Biol. Chem. 273 (23): 14380–6. DOI:10.1074/jbc.273.23.14380. PMID 9603948.
Funakoshi A, Fukamizu Y, Miyasaka K (2000). „Mechanism of cholecystokinin-A- receptor antagonist on human pancreatic exocrine secretion. Localization of CCK-A receptor in the human duodenum.”. Digestion 60 Suppl 1: 75–80. PMID 10026437.
Gigoux V, Escrieut C, Fehrentz JA, et al. (1999). „Arginine 336 and asparagine 333 of the human cholecystokinin-A receptor binding site interact with the penultimate aspartic acid and the C-terminal amide of cholecystokinin.”. J. Biol. Chem. 274 (29): 20457–64. DOI:10.1074/jbc.274.29.20457. PMID 10400673.
Pellegrini M, Mierke DF (1999). „Molecular complex of cholecystokinin-8 and N-terminus of the cholecystokinin A receptor by NMR spectroscopy.”. Biochemistry 38 (45): 14775–83. DOI:10.1021/bi991272l. PMID 10555959.
Gigoux V, Maigret B, Escrieut C, et al. (2000). „Arginine 197 of the cholecystokinin-A receptor binding site interacts with the sulfate of the peptide agonist cholecystokinin.”. Protein Sci. 8 (11): 2347–54. DOI:10.1110/ps.8.11.2347. PMC 2144185. PMID 10595537.
Funakoshi A, Miyasaka K, Matsumoto H, et al. (2000). „Gene structure of human cholecystokinin (CCK) type-A receptor: body fat content is related to CCK type-A receptor gene promoter polymorphism.”. FEBS Lett. 466 (2-3): 264–6. DOI:10.1016/S0014-5793(00)01080-2. PMID 10682840.
Tachikawa H, Harada S, Kawanishi Y, et al. (2000). „Novel polymorphisms of the human cholecystokinin A receptor gene: an association analysis with schizophrenia.”. Am. J. Med. Genet. 96 (2): 141–5. DOI:10.1002/(SICI)1096-8628(20000403)96:2<141::AID-AJMG3>3.0.CO;2-R. PMID 10893485.
Giragossian C, Mierke DF (2001). „Intermolecular interactions between cholecystokinin-8 and the third extracellular loop of the cholecystokinin A receptor.”. Biochemistry 40 (13): 3804–9. DOI:10.1021/bi002659n. PMID 11300760.
Schmitz F, Schrader H, Otte J, et al. (2002). „Identification of CCK-B/gastrin receptor splice variants in human peripheral blood mononuclear cells.”. Regul. Pept. 101 (1-3): 25–33. DOI:10.1016/S0167-0115(01)00281-6. PMID 11495676.
Tachikawa H, Harada S, Kawanishi Y, et al. (2002). „Linked polymorphisms (-333G>T and -286A>G) in the promoter region of the CCK-A receptor gene may be associated with schizophrenia.”. Psychiatry research 103 (2-3): 147–55. DOI:10.1016/S0165-1781(01)00276-1. PMID 11549403.
Schmitz F, Göke MN, Otte JM, et al. (2002). „Cellular expression of CCK-A and CCK-B/gastrin receptors in human gastric mucosa.”. Regul. Pept. 102 (2-3): 101–10. DOI:10.1016/S0167-0115(01)00307-X. PMID 11730982.
Okubo T, Harada S, Higuchi S, Matsushita S (2003). „Investigation of quantitative trait loci in the CCKAR gene with susceptibility to alcoholism.”. Alcohol. Clin. Exp. Res. 26 (8 Suppl): 2S–5S. DOI:10.1097/01.ALC.0000026826.96191.FB. PMID 12198366.
Takata Y, Takeda S, Kawanami T, et al. (2003). „Promoter analysis of human cholecystokinin type-A receptor gene.”. J. Gastroenterol. 37 (10): 815–20. DOI:10.1007/s005350200135. PMID 12424565.

Vanjske veze

„Cholecystokinin Receptors: CCK₁”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2012-10-23.