Receptor glukagonu sličnog peptida 1

Receptor glukagonu sličnog peptida 1‎‎
Receptor glukagonu sličnog peptida 1‎‎
	Prikaz bazira na PDB 3C59.
Dostupne strukture
	3C59, 3C5T, 3IOL
Identifikatori
Simboli	GLP1R; MGC138331
Vanjski ID	OMIM: 138032 MGI: 99571 HomoloGene: 1558 IUPHAR: GLP-1 GeneCards: GLP1R Gene
Ontologija gena
Molekularna funkcija	• aktivnost transmembranskog signalnog receptora; • aktivnost glukagonskog receptora; • aktivnosti G-protein spregnutog peptidnog receptora; • vezivanje peptidnog hormona;
Celularna komponenta	• ćelijska membrana; • integralno sa ćelijskom membranom; • integralno sa membranom;
Biološki proces	• metabolički proces energetske rezerve; • signalni put G-protein spregnutog receptor aktiviranog adenilat ciklazom; • aktivacija adenilat ciklazne aktivnosti;
Pregled RNK izražavanja
	podaci
Ortolozi
Vrsta	Čovek
Entrez	2740
Ensembl	ENSG00000112164
UniProt	P43220
RefSeq (mRNA)	NM_002062.3
RefSeq (protein)	NP_002053.3
Lokacija (UCSC)	Chr 6:; 39.02 - 39.06 Mb
PubMed pretraga	[1]

Receptor glukagonu sličnog peptida 1 (GLP1R) je ljudski gen koji se nalazi na hromozomu 6.^[1]^[2] Ovaj protein je član glukogenske receptorske familije G protein spregnutih receptora.^[3]

Specifičnost liganda

GLP1R specifično vezuje glukagonu sličan peptid-1 (GLP1) i ima mnogo manji afinitet za srodne peptide kao što su gastrični inhibitorni polipeptid i glukagon.^[4]

Funkcija i terapeutski potencijal

GLP1R je izražen u pancreasnim beta ćelijama. Aktivirani GLP1R stimuliše adenilil ciklazni put što dovodi do povišene sinteze i otpuštanja insulina.^[5] Shodno tome, GLP1R je predložen kao potencijalni cilj za lečenje diabetesa.^[6]

GLP1R je isto tako izražen u mozgu gde učestvuje u kontroli apetita.^[7] Miševi kod kojih je GLP1R izrađen u povećanoj meri pokazuju poboljšanu memoriju i sposobnost učenja.^[8]

Reference

^ Thorens B (1992). „Expression cloning of the pancreatic beta cell receptor for the gluco-incretin hormone glucagon-like peptide 1”. Proc. Natl. Acad. Sci. U.S.A. 89 (18): 8641—5. PMC 49976 . PMID 1326760. doi:10.1073/pnas.89.18.8641.
^ Dillon JS, Tanizawa Y, Wheeler MB, Leng XH, Ligon BB, Rabin DU, Yoo-Warren H, Permutt MA, Boyd AE 3rd (1993). „Cloning and functional expression of the human glucagon-like peptide-1 (GLP-1) receptor”. Endocrinology. 133 (4): 1907—10. PMID 8404634. doi:10.1210/en.133.4.1907.
^ Brubaker PL, Drucker DJ (2002). „Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors” (PDF). Recept. Channels. 8 (3-4): 179—88. PMID 12529935. doi:10.1080/10606820213687. Приступљено 14. 07. 2008.
^ Fehmann HC, Jiang J, Schweinfurth J, Dörsch K, Wheeler MB, Boyd AE 3rd, Göke B (1994). „Ligand-specificity of the rat GLP-I receptor recombinantly expressed in Chinese hamster ovary (CHO-) cells”. Z Gastroenterol. 32 (4): 203—7. PMID 8017094.
^ Drucker DJ, Philippe J, Mojsov S, Chick WL, Habener JF (1987). „Glucagon-like peptide I stimulates insulin gene expression and increases cyclic AMP levels in a rat islet cell line”. Proc. Natl. Acad. Sci. U.S.A. 84 (10): 3434—8. PMC 304885 . PMID 3033647. doi:10.1073/pnas.84.10.3434.
^ Holst JJ (2004). „Treatment of type 2 diabetes mellitus with agonists of the GLP-1 receptor or DPP-IV inhibitors”. Expert Opin Emerg Drugs. 9 (1): 155—66. PMID 15155141. doi:10.1517/eoed.9.1.155.32952.
^ Kinzig KP, D'Alessio DA, Seeley RJ (1. 12. 2002). „The diverse roles of specific GLP-1 receptors in the control of food intake and the response to visceral illness”. J. Neurosci. 22 (23): 10470—6. PMID 12451146.
^ During MJ, Cao L, Zuzga DS, Francis JS, Fitzsimons HL, Jiao X, Bland RJ, Klugmann M, Banks WA, Drucker DJ, Haile CN (2003). „Glucagon-like peptide-1 receptor is involved in learning and neuroprotection”. Nat. Med. 9 (9): 1173—9. PMID 12925848. doi:10.1038/nm919.

Literatura

van Eyll B; Lankat-Buttgereit B; Bode HP; et al. (1994). „Signal transduction of the GLP-1-receptor cloned from a human insulinoma”. FEBS Lett. 348 (1): 7—13. PMID 7517895. doi:10.1016/0014-5793(94)00553-2.
Gromada J, Rorsman P, Dissing S, Wulff BS (1995). „Stimulation of cloned human glucagon-like peptide 1 receptor expressed in HEK 293 cells induces cAMP-dependent activation of calcium-induced calcium release”. FEBS Lett. 373 (2): 182—6. PMID 7589461. doi:10.1016/0014-5793(95)01070-U.
Wei Y, Mojsov S (1995). „Tissue-specific expression of the human receptor for glucagon-like peptide-I: brain, heart and pancreatic forms have the same deduced amino acid sequences”. FEBS Lett. 358 (3): 219—24. PMID 7843404. doi:10.1016/0014-5793(94)01430-9.
Lankat-Buttgereit B; Göke R; Stöckmann F; et al. (1994). „Detection of the human glucagon-like peptide 1(7-36) amide receptor on insulinoma-derived cell membranes”. Digestion. 55 (1): 29—33. PMID 8112494. doi:10.1159/000201119.
Graziano MP; Hey PJ; Borkowski D; et al. (1993). „Cloning and functional expression of a human glucagon-like peptide-1 receptor”. Biochem. Biophys. Res. Commun. 196 (1): 141—6. PMID 8216285. doi:10.1006/bbrc.1993.2226.
Stoffel M, Espinosa R, Le Beau MM, Bell GI (1993). „Human glucagon-like peptide-1 receptor gene. Localization to chromosome band 6p21 by fluorescence in situ hybridization and linkage of a highly polymorphic simple tandem repeat DNA polymorphism to other markers on chromosome 6”. Diabetes. 42 (8): 1215—8. PMID 8392011. doi:10.2337/diabetes.42.8.1215.
Dillon JS; Tanizawa Y; Wheeler MB; et al. (1993). „Cloning and functional expression of the human glucagon-like peptide-1 (GLP-1) receptor”. Endocrinology. 133 (4): 1907—10. PMID 8404634. doi:10.1210/en.133.4.1907.
Thorens B; Porret A; Bühler L; et al. (1993). „Cloning and functional expression of the human islet GLP-1 receptor. Demonstration that exendin-4 is an agonist and exendin-(9-39) an antagonist of the receptor”. Diabetes. 42 (11): 1678—82. PMID 8405712. doi:10.2337/diabetes.42.11.1678.
Lankat-Buttgereit B, Göke B (1997). „Cloning and characterization of the 5' flanking sequences (promoter region) of the human GLP-1 receptor gene”. Peptides. 18 (5): 617—24. PMID 9213353. doi:10.1016/S0196-9781(97)00001-6.
Frimurer TM, Bywater RP (1999). „Structure of the integral membrane domain of the GLP1 receptor”. Proteins. 35 (4): 375—86. PMID 10382665. doi:10.1002/(SICI)1097-0134(19990601)35:4<375::AID-PROT1>3.0.CO;2-2.
Huypens P, Ling Z, Pipeleers D, Schuit F (2001). „Glucagon receptors on human islet cells contribute to glucose competence of insulin release”. Diabetologia. 43 (8): 1012—9. PMID 10990079. doi:10.1007/s001250051484.
Hartley JL, Temple GF, Brasch MA (2001). „DNA cloning using in vitro site-specific recombination”. Genome Res. 10 (11): 1788—95. PMC 310948 . PMID 11076863. doi:10.1101/gr.143000.
Xiao Q, Jeng W, Wheeler MB (2001). „Characterization of glucagon-like peptide-1 receptor-binding determinants”. J. Mol. Endocrinol. 25 (3): 321—35. PMID 11116211. doi:10.1677/jme.0.0250321.
Bazarsuren A; Grauschopf U; Wozny M; et al. (2003). „In vitro folding, functional characterization, and disulfide pattern of the extracellular domain of human GLP-1 receptor”. Biophys. Chem. 96 (2-3): 305—18. PMID 12034449. doi:10.1016/S0301-4622(02)00023-6.
Strausberg RL; Feingold EA; Grouse LH; et al. (2003). „Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences”. Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899—903. PMC 139241 . PMID 12477932. doi:10.1073/pnas.242603899.
Mungall AJ; Palmer SA; Sims SK; et al. (2003). „The DNA sequence and analysis of human chromosome 6”. Nature. 425 (6960): 805—11. PMID 14574404. doi:10.1038/nature02055.
Tokuyama Y; Matsui K; Egashira T; et al. (2005). „Five missense mutations in glucagon-like peptide 1 receptor gene in Japanese population”. Diabetes Res. Clin. Pract. 66 (1): 63—9. PMID 15364163. doi:10.1016/j.diabres.2004.02.004.
Gerhard DS; Wagner L; Feingold EA; et al. (2004). „The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)”. Genome Res. 14 (10B): 2121—7. PMC 528928 . PMID 15489334. doi:10.1101/gr.2596504.
Jorgensen R, Martini L, Schwartz TW, Elling CE (2005). „Characterization of glucagon-like peptide-1 receptor beta-arrestin 2 interaction: a high-affinity receptor phenotype”. Mol. Endocrinol. 19 (3): 812—23. PMID 15528268. doi:10.1210/me.2004-0312.
Mahon MJ, Shimada M (2005). „Calmodulin interacts with the cytoplasmic tails of the parathyroid hormone 1 receptor and a sub-set of class b G-protein coupled receptors”. FEBS Lett. 579 (3): 803—7. PMID 15670850. doi:10.1016/j.febslet.2004.12.056.

Vidi još

Spoljašnje veze

„Glucagon Receptor Family: GLP-1”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Архивирано из оригинала 03. 03. 2016. г.
glucagon-like+peptide+receptor на US National Library of Medicine Medical Subject Headings (MeSH)

[pmid1326760-1] Thorens B (1992). „Expression cloning of the pancreatic beta cell receptor for the gluco-incretin hormone glucagon-like peptide 1”. Proc. Natl. Acad. Sci. U.S.A. 89 (18): 8641—5. PMC 49976 . PMID 1326760. doi:10.1073/pnas.89.18.8641.

[pmid8404634-2] Dillon JS, Tanizawa Y, Wheeler MB, Leng XH, Ligon BB, Rabin DU, Yoo-Warren H, Permutt MA, Boyd AE 3rd (1993). „Cloning and functional expression of the human glucagon-like peptide-1 (GLP-1) receptor”. Endocrinology. 133 (4): 1907—10. PMID 8404634. doi:10.1210/en.133.4.1907.

[pmid12529935-3] Brubaker PL, Drucker DJ (2002). „Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors” (PDF). Recept. Channels. 8 (3-4): 179—88. PMID 12529935. doi:10.1080/10606820213687. Приступљено 14. 07. 2008.

[pmid8017094-4] Fehmann HC, Jiang J, Schweinfurth J, Dörsch K, Wheeler MB, Boyd AE 3rd, Göke B (1994). „Ligand-specificity of the rat GLP-I receptor recombinantly expressed in Chinese hamster ovary (CHO-) cells”. Z Gastroenterol. 32 (4): 203—7. PMID 8017094.

[pmid3033647-5] Drucker DJ, Philippe J, Mojsov S, Chick WL, Habener JF (1987). „Glucagon-like peptide I stimulates insulin gene expression and increases cyclic AMP levels in a rat islet cell line”. Proc. Natl. Acad. Sci. U.S.A. 84 (10): 3434—8. PMC 304885 . PMID 3033647. doi:10.1073/pnas.84.10.3434.

[pmid15155141-6] Holst JJ (2004). „Treatment of type 2 diabetes mellitus with agonists of the GLP-1 receptor or DPP-IV inhibitors”. Expert Opin Emerg Drugs. 9 (1): 155—66. PMID 15155141. doi:10.1517/eoed.9.1.155.32952.

[pmid12451146-7] Kinzig KP, D'Alessio DA, Seeley RJ (1. 12. 2002). „The diverse roles of specific GLP-1 receptors in the control of food intake and the response to visceral illness”. J. Neurosci. 22 (23): 10470—6. PMID 12451146.

[pmid12925848-8] During MJ, Cao L, Zuzga DS, Francis JS, Fitzsimons HL, Jiao X, Bland RJ, Klugmann M, Banks WA, Drucker DJ, Haile CN (2003). „Glucagon-like peptide-1 receptor is involved in learning and neuroprotection”. Nat. Med. 9 (9): 1173—9. PMID 12925848. doi:10.1038/nm919.

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