Kortikotropin-oslobađajući hormonski receptor 1

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Kortikotropin-oslobađajući hormonski receptor 1
Identifikatori
SimboliCRHR1; CRF-R; CRF1; CRFR1; CRH-R1h; CRHR1f
Vanjski IDOMIM: 122561 MGI: 88498 HomoloGene: 20920 IUPHAR: CRF1 GeneCards: CRHR1 Gene
Ontologija gena
Molekularna funkcija receptorska aktivnost
aktivnost G-protein spregnutog receptora
aktivnost receptora kortikotropin-oslobađajućeg faktora
Celularna komponenta ćelijska membrana
integralno sa ćelijskom membranom
membrana
Biološki proces respons na stres
imunski respons
prenos signala
signalni put G-protein spregnutog receptora
G-protein signalizacija, spregnuta sa cAMP nukleotidnim sekundarnim glasnikom
aktivacija adenilat ciklaze
trudnoća
porođaj
ponašanje
Pregled RNK izražavanja
podaci
Ortolozi
VrstaČovekMiš
Entrez139412921
EnsemblENSG00000120088ENSMUSG00000018634
UniProtP34998Q0VGH2
RefSeq (mRNA)XM_001128344NM_007762
RefSeq (protein)XP_001128344NP_031788
Lokacija (UCSC)Chr 17:
41.24 - 41.27 Mb
Chr 11:
103.95 - 103.99 Mb
PubMed pretraga[1][2]

Kortikotropin-oslobađajući hormonski receptor 1 (CRHR1, CRF1) je protein koji je kod ljudi kodiran CRHR1 genom.[1][2][3]

Funkcija

Kortikotropin-oslobađajući hormonski receptor vezuje kortikotropin-oslobađajući hormon, potentan posrednik endokrinog, autonomnog, i imunskog responsa na stres.[4]

Kod miševa CRF1 receptori posreduju etanolno pojačanje GABAergične sinaptičke transmisije.[5]

Klinički značaj

Varijacije CRHR1 gena su povezane za povećanjem odgovora na inhalacionu kortikosteroidnu terapiju kod astme.[6] Antagonisti CRF1 receptora se aktivno ispituju kao mogući tretman za depresiju i anksioznost.[7][8]

Interakcije

Za kortikotropin-oslobađajući hormonski receptor 1 je pokazano da interaguje sa kortikotropin-oslobađajućim hormonom[9][10] i urokortinom.[11][10]

Vidi još

Literatura

  1. Hauger RL, Grigoriadis DE, Dallman MF, Plotsky PM, Vale WW, Dautzenberg FM (March 2003). „International Union of Pharmacology. XXXVI. Current status of the nomenclature for receptors for corticotropin-releasing factor and their ligands”. Pharmacol. Rev. 55 (1): 21–6. DOI:10.1124/pr.55.1.3. PMID 12615952. 
  2. Polymeropoulos MH, Torres R, Yanovski JA, Chandrasekharappa SC, Ledbetter DH (July 1995). „The human corticotropin-releasing factor receptor (CRHR) gene maps to chromosome 17q12-q22”. Genomics 28 (1): 123–4. DOI:10.1006/geno.1995.1118. PMID 7590738. 
  3. Chen R, Lewis KA, Perrin MH, Vale WW (October 1993). „Expression cloning of a human corticotropin-releasing-factor receptor”. Proc. Natl. Acad. Sci. U.S.A. 90 (19): 8967–71. DOI:10.1073/pnas.90.19.8967. PMC 47482. PMID 7692441. 
  4. „Entrez Gene: CRHR1 corticotropin releasing hormone receptor 1”. 
  5. Nie Z, Schweitzer P, Roberts AJ, Madamba SG, Moore SD, Siggins GR (March 2004). „Ethanol augments GABAergic transmission in the central amygdala via CRF1 receptors”. Science (journal) 303 (5663): 1512–4. DOI:10.1126/science.1092550. PMID 15001778. 
  6. Tantisira KG, Lake S, Silverman ES, Palmer LJ, Lazarus R, Silverman EK, Liggett SB, Gelfand EW, Rosenwasser LJ, Richter B, Israel E, Wechsler M, Gabriel S, Altshuler D, Lander E, Drazen J, Weiss ST (July 2004). „Corticosteroid pharmacogenetics: association of sequence variants in CRHR1 with improved lung function in asthmatics treated with inhaled corticosteroids”. Hum. Mol. Genet. 13 (13): 1353–9. DOI:10.1093/hmg/ddh149. PMID 15128701. 
  7. Kehne JH (June 2007). „The CRF1 receptor, a novel target for the treatment of depression, anxiety, and stress-related disorders”. CNS Neurol Disord Drug Targets 6 (3): 163–82. DOI:10.2174/187152707780619344. PMID 17511614. 
  8. Ising M, Holsboer F (December 2007). „CRH-sub-1 receptor antagonists for the treatment of depression and anxiety”. Exp Clin Psychopharmacol 15 (6): 519–28. DOI:10.1037/1064-1297.15.6.519. PMID 18179304. 
  9. Grammatopoulos, D K; Dai Y, Randeva H S, Levine M A, Karteris E, Easton A J, Hillhouse E W (December 1999). „A novel spliced variant of the type 1 corticotropin-releasing hormone receptor with a deletion in the seventh transmembrane domain present in the human pregnant term myometrium and fetal membranes”. Mol. Endocrinol. (UNITED STATES) 13 (12): 2189–202. DOI:10.1210/me.13.12.2189. ISSN 0888-8809. PMID 10598591. 
  10. 10,0 10,1 Gottowik, J; Goetschy V, Henriot S, Kitas E, Fluhman B, Clerc R G, Moreau J L, Monsma F J, Kilpatrick G J (October 1997). „Labelling of CRF1 and CRF2 receptors using the novel radioligand, [3H-urocortin”]. Neuropharmacology (ENGLAND) 36 (10): 1439–46. DOI:10.1016/S0028-3908(97)00098-1. ISSN 0028-3908. PMID 9423932. 
  11. Donaldson, C J; Sutton S W, Perrin M H, Corrigan A Z, Lewis K A, Rivier J E, Vaughan J M, Vale W W (May 1996). „Cloning and characterization of human urocortin”. Endocrinology (UNITED STATES) 137 (5): 2167–70. DOI:10.1210/en.137.5.2167. ISSN 0013-7227. PMID 8612563. 

Dodatna literatura

  • Taché Y, Martinez V, Wang L, Million M (2004). „CRF1 receptor signaling pathways are involved in stress-related alterations of colonic function and viscerosensitivity: implications for irritable bowel syndrome.”. Br. J. Pharmacol. 141 (8): 1321–30. DOI:10.1038/sj.bjp.0705760. PMC 1574904. PMID 15100165. 
  • McLean M, Bisits A, Davies J, et al. (1995). „A placental clock controlling the length of human pregnancy.”. Nat. Med. 1 (5): 460–3. DOI:10.1038/nm0595-460. PMID 7585095. 
  • Polymeropoulos MH, Torres R, Yanovski JA, et al. (1995). „The human corticotropin-releasing factor receptor (CRHR) gene maps to chromosome 17q12-q22.”. Genomics 28 (1): 123–4. DOI:10.1006/geno.1995.1118. PMID 7590738. 
  • Chen R, Lewis KA, Perrin MH, Vale WW (1993). „Expression cloning of a human corticotropin-releasing-factor receptor.”. Proc. Natl. Acad. Sci. U.S.A. 90 (19): 8967–71. DOI:10.1073/pnas.90.19.8967. PMC 47482. PMID 7692441. 
  • Ross PC, Kostas CM, Ramabhadran TV (1995). „A variant of the human corticotropin-releasing factor (CRF) receptor: cloning, expression and pharmacology.”. Biochem. Biophys. Res. Commun. 205 (3): 1836–42. DOI:10.1006/bbrc.1994.2884. PMID 7811272. 
  • Opdenakker G, Fiten P, Nys G, et al. (1994). „The human MCP-3 gene (SCYA7): cloning, sequence analysis, and assignment to the C-C chemokine gene cluster on chromosome 17q11.2-q12.”. Genomics 21 (2): 403–8. DOI:10.1006/geno.1994.1283. PMID 7916328. 
  • Vita N, Laurent P, Lefort S, et al. (1993). „Primary structure and functional expression of mouse pituitary and human brain corticotrophin releasing factor receptors.”. FEBS Lett. 335 (1): 1–5. DOI:10.1016/0014-5793(93)80427-V. PMID 8243652. 
  • Donaldson CJ, Sutton SW, Perrin MH, et al. (1996). „Cloning and characterization of human urocortin.”. Endocrinology 137 (5): 2167–70. DOI:10.1210/en.137.5.2167. PMID 8612563. 
  • Liaw CW, Grigoriadis DE, Lovenberg TW, et al. (1997). „Localization of ligand-binding domains of human corticotropin-releasing factor receptor: a chimeric receptor approach.”. Mol. Endocrinol. 11 (7): 980–5. DOI:10.1210/me.11.7.980. PMID 9178757. 
  • Asakura H, Zwain IH, Yen SS (1997). „Expression of genes encoding corticotropin-releasing factor (CRF), type 1 CRF receptor, and CRF-binding protein and localization of the gene products in the human ovary.”. J. Clin. Endocrinol. Metab. 82 (8): 2720–5. DOI:10.1210/jc.82.8.2720. PMID 9253360. 
  • Gottowik J, Goetschy V, Henriot S, et al. (1998). „Labelling of CRF1 and CRF2 receptors using the novel radioligand, [3H]-urocortin.”. Neuropharmacology 36 (10): 1439–46. DOI:10.1016/S0028-3908(97)00098-1. PMID 9423932. 
  • Grammatopoulos D, Dai Y, Chen J, et al. (1998). „Human corticotropin-releasing hormone receptor: differences in subtype expression between pregnant and nonpregnant myometria.”. J. Clin. Endocrinol. Metab. 83 (7): 2539–44. DOI:10.1210/jc.83.7.2539. PMID 9661640. 
  • Sakai K, Yamada M, Horiba N, et al. (1998). „The genomic organization of the human corticotropin-releasing factor type-1 receptor.”. Gene 219 (1-2): 125–30. DOI:10.1016/S0378-1119(98)00322-9. PMID 9757017. 
  • Grammatopoulos DK, Dai Y, Randeva HS, et al. (2000). „A novel spliced variant of the type 1 corticotropin-releasing hormone receptor with a deletion in the seventh transmembrane domain present in the human pregnant term myometrium and fetal membranes.”. Mol. Endocrinol. 13 (12): 2189–202. DOI:10.1210/me.13.12.2189. PMID 10598591. 
  • Lewis K, Li C, Perrin MH, et al. (2001). „Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor.”. Proc. Natl. Acad. Sci. U.S.A. 98 (13): 7570–5. DOI:10.1073/pnas.121165198. PMC 34709. PMID 11416224. 
  • Perrin MH, Fischer WH, Kunitake KS, et al. (2001). „Expression, purification, and characterization of a soluble form of the first extracellular domain of the human type 1 corticotropin releasing factor receptor.”. J. Biol. Chem. 276 (34): 31528–34. DOI:10.1074/jbc.M101838200. PMID 11425856. 
  • Pisarchik A, Slominski AT (2002). „Alternative splicing of CRH-R1 receptors in human and mouse skin: identification of new variants and their differential expression.”. FASEB J. 15 (14): 2754–6. DOI:10.1096/fj.01-0487fje. PMID 11606483. 
  • Graziani G, Tentori L, Portarena I, et al. (2002). „CRH inhibits cell growth of human endometrial adenocarcinoma cells via CRH-receptor 1-mediated activation of cAMP-PKA pathway.”. Endocrinology 143 (3): 807–13. DOI:10.1210/en.143.3.807. PMID 11861501. 
  • 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. DOI:10.1073/pnas.242603899. PMC 139241. PMID 12477932. 
  • King JS, Bishop GA (2003). „The distribution and cellular localization of CRF-R1 in the vermis of the postnatal mouse cerebellum.”. Exp. Neurol. 178 (2): 175–85. DOI:10.1006/exnr.2002.8052. PMID 12504877. 

Spoljašnje veze

  • „Corticotropin-releasing Factor Receptors: CRF1”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2015-11-20. 
  • MeSH CRF+receptor+type+1
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Klasa A: Rodopsinu slični
α1 (A, B, D) • α2 (A, B, C) • β1 • β2 • β3
Adenozinski (A1, A2A, A2B, A3) • P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(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
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
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 ne σ) • 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
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
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Drugi
Klasa C: Metabotropni
glutamat / feromon
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
Klasa F:
Frizzled / Zaglađeni
Uvojiti
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
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)
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Neuropeptidni receptori
Hormonski receptori
Drugi
Opioidni receptori
Drugi neuropeptidni receptori
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)
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Holecistokinin
CCKA
Agonisti: Holecistokinin • CCK-4
Antagonisti: Asperlicin • Proglumid • Lorglumid • Devazepid • Deksloksiglumid
CCKB
Agonisti: Holecistokinin • CCK-4 • Gastrin
Antagonisti: Proglumid • CI-988
CRH
CRF1
CRF2
Galanin
GAL1
Agonisti: Galanin • Galaninu-sličan peptid • Galmic • Galnon
GAL2
Agonisti: Galanin • Galaninu-sličan peptid • Galmic • Galnon
GAL3
Agonisti: Galanin • Galmic • Galnon
Grelin
Agonisti: Grelin • Kapromorelin • MK-677 • Sermorelin • SM-130,686 • Tabimorelin
MCH
MCH1
MCH2
Melanokortin
MC1
MC2
Agonisti: ACTH • Kosintropin • Tetrakosaktid
MC3
Agonisti: alfa-MSH • Bremelanotid • Melanotan II
MC4
Agonisti: alfa-MSH • Bremelanotid • Melanotan II • THIQ
Antagonisti: Agutiju srodni peptid
MC5
Agonisti: alfa-MSH • Melanotan II
Neuropeptid S
Agonisti: Neuropeptid S
Antagonisti: SHA-68
Neuropeptid Y
Y1
Agonisti: Neuropeptid Y • Peptid YY
Antagonisti: BIBP-3226
Y2
Agonisti: Neuropeptid Y • Peptid YY
Antagonisti: BIIE-0246
Y4
Agonisti: Neuropeptid Y • Pankreasni polipeptid • Peptid YY
Antagonisti: UR-AK49
Y5
Agonisti: Neuropeptid Y • Peptid YY
Antagonisti: Lu AA-33810
Neurotenzin
NTS1
Agonisti: Neurotenzin • Neuromedin N
Antagonisti: SR-48692 • SR-142,948
NTS2
Agonisti: Neurotenzin
Antagonisti: Levokabastin • SR-142,948
Opioid
vidi Opioidi
Oreksin
OX1
Agonisti: Oreksin-A
Antagonisti: Almoreksant • SB-334,867 • SB-408,124 • SB-649,868
OX2
Agonisti: Oreksin-A
Antagonisti: Almoreksant • SB-649,868 • TCS-OX2-29
Oksitocin
Agonisti: Karbetocin • Demoksitocin • Oksitocin • WAY-267,464
Antagonisti: Atosiban • L-371,257 • L-368,899
Tahikinin
NK1
Agonisti: Supstanca P
Antagonisti: Aprepitant • Befetupitant • Kasopitant • CI-1021 • CP-96,345 • CP-99,994 • CP-122,721 • Dapitant • Ezlopitant • FK-888 • Fosaprepitant • GR-203,040 • GW-597,599 • HSP-117 • L-733,060 • L-741,671 • L-743,310 • L-758,298 • Lanepitant • LY-306,740 • Maropitant • Netupitant • NKP-608 • Nolpitantium • Orvepitant • RP-67,580 • SDZ NKT 343 • Vestipitant • Vofopitant
NK2
Agonisti: Neurokinin A
Antagonisti: GR-159897 • Ibodutant • Saredutant
NK3
Agonisti: Neurokinin B
Antagonisti: Osanetant • Talnetant
Vazopresin
V1A
Agonisti: Dezmopresin • Felipresin • Ornipresin • Terlipresin • Vazopresin
Antagonisti: Konivaptan • Demeklociklin • Relkovaptan
V1B
Agonisti: Felipresin • Ornipresin • Terlipresin • Vazopresin
Antagonisti: Demeklociklin • Nelivaptan
V2
Agonisti: Dezmopresin • Ornipresin • Vazopresin
Antagonisti: Konivaptan • Demeklociklin • Liksivaptan • Mozavaptan • Satavaptan • Tolvaptan