Melatoninski receptor 1B

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Melatoninski receptor 1B
Identifikatori
SimboliMTNR1B; FGQTL2; MEL-1B-R; MT2
Vanjski IDOMIM600804 MGI2181726 HomoloGene4350 IUPHAR: MT2 GeneCards: MTNR1B Gene
Pregled RNK izražavanja
PBB GE MTNR1B 208516 at tn.png
podaci
Ortolozi
VrstaČovekMiš
Entrez4544244701
EnsemblENSG00000134640ENSMUSG00000050901
UniProtP49286Q3SXF8
RefSeq (mRNA)NM_005959.3NM_145712.2
RefSeq (protein)NP_005950.1NP_663758.2
Lokacija (UCSC)Chr 11:
92.7 - 92.72 Mb
Chr 9:
15.67 - 15.68 Mb
PubMed pretraga[1][2]

Melatoninski receptor 1B (MTNR1B) je protein koji je kod ljudi kodiran MTNR1B genom.[1][2]

Funkcija[uredi - уреди | uredi izvor]

MT2 protein je jedan od dve forme receptora sa visokim afinitetom za melatonin, primarni hormon epifize. On je integralni membranski protein koji je G protein spregnuti receptor, 7-transmembranski receptor. On je prisutan prvenstveno u retini i mozgu. Smatra se da on učestvuje u od svetla zavisnim funkcijama u retini i da posreduje neurobiološke efekte melatonina.[1]

Klinički značaj[uredi - уреди | uredi izvor]

Nekoliko studija je identifikovalo da su mutacije MTNR1B receptora vezane za povišeni prosečne nivoe krvnog šećera, i za oko 20 procenata povišen rizik razvoja tip 2 dijabetesa.[3][4][5] MTNR1B iRNK je izražena u ljudskim Langerhansovim ostrvcima, i imunocitohemija potvrđuje da je prvenstveno lociran u beta ćelijama.[4]

MT2R ligandi[uredi - уреди | uredi izvor]

Sledeći MT2R ligandi su selektivni u odnosu na MT1R:

  • Jedinjenje 3d: antagonist sa sub-nM afinitetom[6]
  • Jedinjenje 18f: antagonist i jedinjenje 18g parcijalni agonist: sub-nM afinitet, >100-puta selektivniji u odnosu na MT1[7]
  • Jedinjenje 14: antagonist[8]
  • Jedinjenje 13: agonist[9]

Reference[uredi - уреди | uredi izvor]

  1. 1,0 1,1 "Entrez Gene: MTNR1B melatonin receptor 1B". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=4544. 
  2. Reppert SM, Godson C, Mahle CD, Weaver DR, Slaugenhaupt SA, Gusella JF (September 1995). "Molecular characterization of a second melatonin receptor expressed in human retina and brain: the Mel1b melatonin receptor". Proc. Natl. Acad. Sci. U.S.A. 92 (19): 8734–8. PMC 41041. PMID 7568007. doi:10.1073/pnas.92.19.8734. 
  3. "Gene That Regulates Glucose Levels And Increases Risk For Diabetes Identified". ScienceDaily. 28. 06. 2008.. http://www.sciencedaily.com/releases/2008/06/080609085957.htm. pristupljeno 18. 01. 2009.. ; "Body Clock Linked To Diabetes And High Blood Sugar In New Genome-wide Study". ScienceDaily. 08. 12. 2008.. http://www.sciencedaily.com/releases/2008/12/081207133817.htm. pristupljeno 18. 01. 2009.. ; "Is There A Relationship Between Sleep-wake Rhythm And Diabetes? A New Gene Variant Influences Fasting Glucose Levels Via The Melatonin Metabolism". ScienceDaily. 16. 01. 2009.. http://www.sciencedaily.com/releases/2009/01/090116073601.htm. pristupljeno 18. 01. 2009.. 
  4. 4,0 4,1 Prokopenko I, Langenberg C, Florez JC et al. (January 2009). "Variants in MTNR1B influence fasting glucose levels". Nat. Genet. 41 (1): 77–81. PMC 2682768. PMID 19060907. doi:10.1038/ng.290.  ; Lyssenko V, Nagorny CL, Erdos MR et al. (January 2009). "Common variant in MTNR1B associated with increased risk of type 2 diabetes and impaired early insulin secretion". Nat. Genet. 41 (1): 82–8. PMID 19060908. doi:10.1038/ng.288.  ; Bouatia-Naji N, Bonnefond A, Cavalcanti-Proença C et al. (January 2009). "A variant near MTNR1B is associated with increased fasting plasma glucose levels and type 2 diabetes risk". Nat. Genet. 41 (1): 89–94. PMID 19060909. doi:10.1038/ng.277. 
  5. Staiger H, Machicao F, Schäfer SA et al. (2008). Maedler, Kathrin, ed. "Polymorphisms within the novel type 2 diabetes risk locus MTNR1B determine beta-cell function". PLoS ONE 3 (12): e3962. PMC 2597741. PMID 19088850. doi:10.1371/journal.pone.0003962. 
  6. Rivara S, Lodola A, Mor M et al. (2007). "N-(substituted-anilinoethyl)amides: design, synthesis, and pharmacological characterization of a new class of melatonin receptor ligands". J. Med. Chem. 50 (26): 6618–26. PMID 18052314. doi:10.1021/jm700957j. 
  7. Bedini A, Spadoni G, Gatti G et al. (2006). "Design and synthesis of N-(3,3-diphenylpropenyl)alkanamides as a novel class of high-affinity MT2-selective melatonin receptor ligands". J. Med. Chem. 49 (25): 7393–403. PMID 17149869. doi:10.1021/jm060850a. 
  8. Yous S, Durieux-Poissonnier S, Lipka-Belloli E et al. (2003). "Design and synthesis of 3-phenyl tetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands". Bioorg. Med. Chem. 11 (5): 753–9. PMID 12538005. doi:10.1016/S0968-0896(02)00473-X. 
  9. Mattson RJ, Catt JD, Keavy D et al. (2003). "Indanyl piperazines as melatonergic MT2 selective agents". Bioorg. Med. Chem. Lett. 13 (6): 1199–202. PMID 12643943. doi:10.1016/S0960-894X(03)00090-8. 

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