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Niacinski receptor 1

Uredi veze

Izvor: Wikipedija

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Niacinski receptor 1

Identifikatori

Simboli

NIACR1; GPR109A; PUMAG; Puma-g; HM74a; HM74b

Vanjski ID

OMIM: 609163MGI: 1933383HomoloGene: 4391IUPHAR:GeneCards:NIACR1 Gene

Ontologija gena
Molekularna funkcija	•aktivnost rodopsinu sličnog receptora•receptorska aktivnost•GTP vezivanje•aktivnost purinergičkog nukleotidnog receptora, G-protein spregnutog
Celularna komponenta	•integralno sa ćelijskom membranom•membrana
Biološki proces	•prenos signal•signalni put G-protein spregnutog receptora

Ortolozi

Vrsta

Čovek

Miš

RefSeq (mRNA)

RefSeq (protein)

Lokacija (UCSC)

Chr 12:
121.75 - 121.75 Mb

Chr 5:
124.12 - 124.13 Mb

PubMed pretraga

[1]

[2]

Niacinski receptor 1, takođe poznat kaoNIACR1 iliGPR109A, jeprotein koji je kod čoveka kodiranNIACR1genom.^[1]^[2]^[3]^[4]

Funkcija

[uredi |uredi kod]

GPR109A receptor ima visok afinitet zanikotinsku kiselinu (niacin)^[3]^[4]. On je član grupeGPCRreceptora nikotinske kiseline (drugi član jeGPR109B).

GPR109A jeG_i /G_o protein-spregnuti receptor.^[3]

Klinički značaj

[uredi |uredi kod]

Za GPR109A se smatra da jebiomolekulska meta niacina, koji je široko propisivani lek za tretmandislipidemije, i za povišenje nivoaHDL holesterola. Terapeutski učinak niacina je ograničenispiranjem.^[5] Kod GPR109Anokaut miševa, efekti nijacina na lipide^[6] i ispiranje^[7] su eliminisani. Kodarestin beta 1 nokaut miševa, niacinski efekat na ispiranje je znatno umanjen dok je njegov uticaj na lipidne promene zadržan.^[8]

Precizni mehanizam dejstva niacinskih terapeutskih efekata nije potpuno istražen. Smatra se da on delom deluje putem aktivacije GPR109A, što umanjuje nivoe intracelularnogcAMP i time se inhibiralipolizu adipocitima.^[9] U kontrastu s tim, efekat ispiranja je posledica GPR109A aktivacijeERK 1/2 MAP kinaza^[10] posredovanog arestinom beta 1.^[8] Aktivacija MAP kinaza zatim izaziva oslobađanjeprostaglandina D2 izLangerhanovih ćelija kože.^[11]

Literatura

[uredi |uredi kod]

↑Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S (June 2002). „Identification of G protein-coupled receptor genes from the human genome sequence”. FEBS Letters 520 (1-3): 97–101. DOI:10.1016/S0014-5793(02)02775-8. PMID 12044878.
↑„Entrez Gene: GPR109A G protein-coupled receptor 109A”.
↑^3,0^3,1^3,2Wise A, Foord SM, Fraser NJ, Barnes AA, Elshourbagy N, Eilert M, Ignar DM, Murdock PR, Steplewski K, Green A, Brown AJ, Dowell SJ, Szekeres PG, Hassall DG, Marshall FH, Wilson S, Pike NB (March 2003). „Molecular identification of high and low affinity receptors for nicotinic acid”. The Journal of Biological Chemistry 278 (11): 9869–74. DOI:10.1074/jbc.M210695200. PMID 12522134.
↑^4,0^4,1Soga T, Kamohara M, Takasaki J, Matsumoto S, Saito T, Ohishi T, Hiyama H, Matsuo A, Matsushime H, Furuichi K (March 2003). „Molecular identification of nicotinic acid receptor”. Biochemical and Biophysical Research Communications 303 (1): 364–9. DOI:10.1016/S0006-291X(03)00342-5. PMID 12646212.
↑Pike NB (December 2005). „Flushing out the role of GPR109A (HM74A) in the clinical efficacy of nicotinic acid”. The Journal of Clinical Investigation 115 (12): 3400–3. DOI:10.1172/JCI27160. PMC 1297267. PMID 16322787.
↑Tunaru S, Kero J, Schaub A, Wufka C, Blaukat A, Pfeffer K, Offermanns S (March 2003). „PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect”. Nature Medicine 9 (3): 352–5. DOI:10.1038/nm824. PMID 12563315.
↑Benyó Z, Gille A, Kero J, Csiky M, Suchánková MC, Nüsing RM, Moers A, Pfeffer K, Offermanns S (December 2005). „GPR109A (PUMA-G/HM74A) mediates nicotinic acid-induced flushing”. The Journal of Clinical Investigation 115 (12): 3634–40. DOI:10.1172/JCI23626. PMC 1297235. PMID 16322797.
↑^8,0^8,1Walters RW, Shukla AK, Kovacs JJ, Violin JD, Dewire SM, Lam CM, Chen JR, Muehlbauer MJ, Whalen EJ, Lefkowitz RJ (April 2009). „beta-Arrestin1 mediates nicotinic acid-induced flushing, but not its antilipolytic effect, in mice”. The Journal of Clinical Investigation. DOI:10.1172/JCI36806. PMID 19349687.
↑Zhang Y, Schmidt RJ, Foxworthy P, Emkey R, Oler JK, Large TH, Wang H, Su EW, Mosior MK, Eacho PI, Cao G (August 2005). „Niacin mediates lipolysis in adipose tissue through its G-protein coupled receptor HM74A”. Biochemical and Biophysical Research Communications 334 (2): 729–32. DOI:10.1016/j.bbrc.2005.06.141. PMID 16018973.
↑Richman JG, Kanemitsu-Parks M, Gaidarov I, Cameron JS, Griffin P, Zheng H, Guerra NC, Cham L, Maciejewski-Lenoir D, Behan DP, Boatman D, Chen R, Skinner P, Ornelas P, Waters MG, Wright SD, Semple G, Connolly DT (June 2007). „Nicotinic acid receptor agonists differentially activate downstream effectors”. The Journal of Biological Chemistry 282 (25): 18028–36. DOI:10.1074/jbc.M701866200. PMID 17452318.
↑Tang Y, Zhou L, Gunnet JW, Wines PG, Cryan EV, Demarest KT (June 2006). „Enhancement of arachidonic acid signaling pathway by nicotinic acid receptor HM74A”. Biochemical and Biophysical Research Communications 345 (1): 29–37. DOI:10.1016/j.bbrc.2006.04.051. PMID 16674924.

Vanjske veze

[uredi |uredi kod]

„Nicotinic Acid Receptor Family: GPR109A”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano izoriginala na datum 2015-02-23.

Transmembranski receptor:G protein spregnuti receptori

Klasa A:Rodopsinu slični

Neurotransmiter

Adrenergički	α1 (A,B,D) • α2 (A,B,C) • β1 • β2 • β3
Purinski	Adenozinski (A1,A2A,A2B,A3) • P2Y (1,2,4,5,6,8,9,10,11,12,13,14)
Serotoninski	(svi osim 5-HT3)5-HT1 (A,B,D,E,F) • 5-HT2 (A,B,C) • 5-HT (4,5A,6,7)
Drugi	Acetilholin (M1,M2,M3,M4,M5) • Dopamin (D1,D2,D3,D4,D5) • Histamin (H1,H2,H3,H4) • Melatonin (1A,1B,1C) • TAAR (1,2,3,5,6,8,9)

Metaboliti i
signalni molekuli

Eikozanoidni	CysLT (1,2) • LTB4 (1,2) • FPRL1 • OXE • Prostaglandin (DP (1,2),EP (1,2,3,4),FP) • Prostaciklin • Tromboksan
Drugi	Žučna kiselina • Kanabinoidni (CB1,CB2,GPR (18,55,119)) • EBI2 • Estrogen • Slobodna masna kiselina (1,2,3,4) • Laktat • Lizofosfatidna kiselina (1,2,3,4,5,6) • Lizofosfolipid (1,2,3,4,5,6,7,8) • Niacin (1,2) • Oksoglutarat • PAF • Sfingozin-1-fosfat (1,2,3,4,5) • Sukcinat

Peptid

Neuropeptidni

B/W (1,2) • FF (1,2) • S • Y (1,2,4,5) • Neuromedin (B,U (1,2)) • Neurotenzin (1,2)

Drugi

Anafilatoksin (C3a,C5a) • Angiotenzin (1,2) • Apelin • Bombezin (BRS3,GRPR,NMBR) • Bradikinin (B1,B2) • Hemokin • Holecistokinin (A,B) • Endotelin (A,B) • Formil peptid (1,2,3) • FSH • Galanin (1,2,3) • GHB receptor • Gonadotropin-oslobađajući hormon (1,2) • Grelin • Kispeptin • Luteinizirajući hormon/horiogonadotropin • MAS (1,1L,D,E,F,G,X1,X2,X3,X4) • Melanokortin (1,2,3,4,5) • MCHR (1,2) • Motilin • Opioidni (δ,κ,μ,Nociceptin &ζ, ali neσ) • Oreksin (1,2) • Oksitocin • Prokineticin (1,2) • Prolaktin-oslobađajući peptid • Relaksin (1,2,3,4) • Somatostatin (1,2,3,4,5) • Tahikinin (1,2,3) • Tirotropin • Tirotropin-oslobađajući hormon • Urotenzin-II • Vazopresin (1A,1B,2)

Razno

Orfan	GPR (1,3,4,6,12,15,17,18,19,20,21,22,23,25,26,27,31,32,33,34,35,37,39,42,44,45,50,52,55,61,62,63,65,68,75,77,78,81,82,83,84,85,87,88,92,101,103,109A,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)
Drugi	Adrenomedulin • Mirisni • Opsin (3,4,5,1LW,1MW,1SW,RGR,RRH) • Proteazom-aktivirani (1,2,3,4) • SREB (1,2,3)

Klasa B:Sekretinu slični

Orfan

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

Drugi

Moždano specifični angiogenezni inhibitor (1,2,3) • Cadherin (1,2,3) • Kalcitonin • CALCRL • CD97 • Kortikotropin-oslobađajući hormon (1,2) • EMR (1,2,3) • Glukagon (GR,GIPR,GLP1R,GLP2R) • Hormon rasta oslobađajući hormon • PACAPR1 • GPR • Latrofilin (1,2,3,ELTD1) • Metuselah-slični proteini • Paratiroidni hormon (1,2) • Sekretin • Vazoaktivni intestinalni peptid (1,2)

Klasa C:Metabotropni
glutamat /feromon

Ukus	TAS1R (1,2,3) • TAS2R (1,3,4,5,8,9,10,12,13,14,16,19,20,30,31,38,39,40,41,42,43,45,46,50)
Drugi	Kalcijum-detektujući receptor • GABA B (1,2) • Glutamatni receptor (Metabotropni glutamat (1,2,3,4,5,6,7,8)) • GPRC6A • GPR (156,158,179) • RAIG (1,2,3,4)

Klasa F:
Frizzled /Zaglađeni

Uvojiti	Frizzled (1,2,3,4,5,6,7,8,9,10)
Zaglađeni	Zaglađeni

B trdu:peptidi (nrpl/grfl/cytl/horl),receptori (lgic,enzr,gprc,igsr,intg,nrpr/grfr/cytr),itra (adap,gbpr,mapk),calc,lipd, signalni putevi (hedp,wntp,tgfp+mapp,notp,jakp,fsap,hipp,tlrp)

Izvor:https://sh.wikipedia.org/w/index.php?title=Niacinski_receptor_1&oldid=42506588

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