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Galaninski receptor

С Википедије, слободне енциклопедије
Galaninski receptor 1
Identifikatori
SimbolGALR1
Alt. simboliGALNR1, GALNR
Entrez2587
HUGO4132
OMIM600377
RefSeqNM_001480
UniProtP47211
Ostali podaci
LokusHromozom 18 q23
Galaninski receptor 2
Identifikatori
SimbolGALR2
Entrez8811
HUGO4133
OMIM603691
RefSeqNM_003857
UniProtO43603
Ostali podaci
LokusHromozom 17 q25.3
Galaninski receptor 3
Identifikatori
SimbolGALR3
Entrez8484
HUGO4134
OMIM603692
RefSeqNM_003614
UniProtO60755
Ostali podaci
LokusHromozom 22 q12.2-13.1

Galaninski receptor je G protein-spregnuti receptor, ili metabotropni receptor koji vezuje galanin.[1]

Galaninski receptori se mogu naći u perifernom i centralnom nervnom sistemu kao i u endokrinom sistemu. Do sada je poznato da postoje tri tipa: GAL-R1, GAL-R2, i GAL-R3.[2] Specifična funkcija svih podtipova nije potpuno istražena. Nedavno je došlo do napretka u pravljenju podtip-specifičnih nokaut miševa,[3][4] i prvih selektivnih liganda galaninskih receptorskih podtipova. Selektivni galaninski agonisti su antiepileptici,[5][6][7] dok su antagonisti antidepresanti i anksiolitici u životinjskim studijama,[8][9][10][11][12], tako da bilo agonisti ili antagonisti galaninskog receptora mogu potencijalno biti lekovi.

Ligandi

[уреди | уреди извор]
===Agonisti===
Neselektivni
GAL1 selektivni
  • M617 peptid
GAL2 selektivni
  • Galanin 2-11 amid - takođe poznat kao AR-M 1896, antikonvulziv kod miševa, CAS# 367518-31-8
  • M1145 - selektivan u odnosu na GalR1 i GalR3[17]

Antagonisti

Neselektivni
  • M35 peptid
GAL1 selektivni
  • SCH-202,596
GAL2 selektivni
  • M871 peptid
GAL3 selektivni

Literatura

[уреди | уреди извор]
  1. ^ Lang R, Gundlach AL, Kofler B (2007). . „The galanin peptide family: receptor pharmacology, pleiotropic biological actions, and implications in health and disease”. Pharmacol. Ther.. 115 (2): 177—207. PMID 17604107. doi:10.1016/j.pharmthera.2007.05.009. 
  2. ^ Branchek TA, Smith KE, Gerald C, Walker MW (2000). . „Galanin receptor subtypes”. Trends Pharmacol. Sci.. 21 (3): 109—17. PMID 10689365. doi:10.1016/S0165-6147(00)01446-2. 
  3. ^ Rustay NR, Wrenn CC, Kinney JW, Holmes A, Bailey KR, Sullivan TL, Harris AP, Long KC, Saavedra MC, Starosta G, Innerfield CE, Yang RJ, Dreiling JL, Crawley JN (2005). . „Galanin impairs performance on learning and memory tasks: findings from galanin transgenic and GAL-R1 knockout mice”. Neuropeptides. 39 (3): 239—43. PMID 15944016. doi:10.1016/j.npep.2004.12.026. 
  4. ^ Lu X, Ross B, Sanchez-Alavez M, Zorrilla EP, Bartfai T (2008). . „Phenotypic analysis of GalR2 knockout mice in anxiety- and depression-related behavioral tests”. Neuropeptides. 42 (4): 387—97. PMID 18554714. doi:10.1016/j.npep.2008.04.009. 
  5. ^ Mazarati A, Lundström L, Sollenberg U, Shin D, Langel U, Sankar R (2006). . „Regulation of kindling epileptogenesis by hippocampal galanin type 1 and type 2 receptors: The effects of subtype-selective agonists and the role of G-protein-mediated signaling”. The Journal of Pharmacology and Experimental Therapeutics. 318 (2): 700—8. PMC 1508166 Слободан приступ. PMID 16699066. doi:10.1124/jpet.106.104703. 
  6. ^ Lerner JT, Sankar R, Mazarati AM (2008). . „Galanin and epilepsy”. Cellular and Molecular Life Sciences : CMLS. 65 (12): 1864—71. PMID 18500639. doi:10.1007/s00018-008-8161-8. 
  7. ^ Zhang L, Robertson CR, Green BR, Pruess TH, White HS, Bulaj G (2009). . „Structural Requirements for a Lipoamino Acid in Modulating the Anticonvulsant Activities of Systemically Active Galanin Analogues”. Journal of Medicinal Chemistry. 52 (5): 1310—6. PMC 2765488 Слободан приступ. PMID 19199479. doi:10.1021/jm801397w. 
  8. ^ Lu X, Barr AM, Kinney JW, Sanna P, Conti B, Behrens MM, Bartfai T (2005). . „A role for galanin in antidepressant actions with a focus on the dorsal raphe nucleus”. Proceedings of the National Academy of Sciences of the United States of America. 102 (3): 874—9. PMC 545581 Слободан приступ. PMID 15647369. doi:10.1073/pnas.0408891102. 
  9. ^ Barr AM, Kinney JW, Hill MN, Lu X, Biros S, Rebek J, Bartfai T (2006). . „A novel, systemically active, selective galanin receptor type-3 ligand exhibits antidepressant-like activity in preclinical tests”. Neuroscience Letters. 405 (1-2): 111—5. PMID 16854525. doi:10.1016/j.neulet.2006.06.033. 
  10. ^ Lu X, Sharkey L, Bartfai T (2007). . „The brain galanin receptors: targets for novel antidepressant drugs”. CNS & Neurological Disorders Drug Targets. 6 (3): 183—92. PMID 17511615. doi:10.2174/187152707780619335. 
  11. ^ Kuteeva E, Hökfelt T, Wardi T, Ogren SO (2008). . „Galanin, galanin receptor subtypes and depression-like behaviour”. Cellular and Molecular Life Sciences : CMLS. 65 (12): 1854—63. PMID 18500640. doi:10.1007/s00018-008-8160-9. 
  12. ^ Kuteeva E, Wardi T, Lundström L, Sollenberg U, Langel U, Hökfelt T, Ogren SO (2008). . „Differential role of galanin receptors in the regulation of depression-like behavior and monoamine/stress-related genes at the cell body level”. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 33 (11): 2573—85. PMID 18172432. doi:10.1038/sj.npp.1301660. 
  13. ^ Ceide SC, Trembleau L, Haberhauer G, Somogyi L, Lu X, Bartfai T, Rebek J (2004). . „Synthesis of galmic: a nonpeptide galanin receptor agonist”. Proceedings of the National Academy of Sciences of the United States of America. 101 (48): 16727—32. PMC 534730 Слободан приступ. PMID 15557002. doi:10.1073/pnas.0407543101. 
  14. ^ Rajarao SJ, Platt B, Sukoff SJ, Lin Q, Bender CN, Nieuwenhuijsen BW, Ring RH, Schechter LE, Rosenzweig-Lipson S, Beyer CE (2007). . „Anxiolytic-like activity of the non-selective galanin receptor agonist, galnon”. Neuropeptides. 41 (5): 307—20. PMID 17637475. doi:10.1016/j.npep.2007.05.001. 
  15. ^ Bulaj G, Green BR, Lee HK, Robertson CR, White K, Zhang L, Sochanska M, Flynn SP, Scholl EA, Pruess TH, Smith MD, White HS (2008). . „Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities”. Journal of Medicinal Chemistry. 51 (24): 8038—47. PMID 19053761. doi:10.1021/jm801088x. 
  16. ^ White HS, Scholl EA, Klein BD, Flynn SP, Pruess TH, Green BR, Zhang L, Bulaj G (2009). . „Developing novel antiepileptic drugs: characterization of NAX 5055, a systemically-active galanin analog, in epilepsy models”. Neurotherapeutics : the Journal of the American Society for Experimental NeuroTherapeutics. 6 (2): 372—80. PMID 19332332. doi:10.1016/j.nurt.2009.01.001. 
  17. ^ Runesson J, Saar I, Lundström L, Järv J, Langel U (2009). . „A novel GalR2-specific peptide agonist”. Neuropeptides. 43 (3): 187—92. PMID 19467704. doi:10.1016/j.npep.2009.04.004. 
  18. ^ Ogren SO, Kuteeva E, Hökfelt T, Kehr J (2006). . „Galanin receptor antagonists : a potential novel pharmacological treatment for mood disorders”. CNS Drugs. 20 (8): 633—54. PMID 16863269. 
  19. ^ Swanson CJ, Blackburn TP, Zhang X, Zheng K, Xu ZQ, Hökfelt T, Wolinsky TD, Konkel MJ, Chen H, Zhong H, Walker MW, Craig DA, Gerald CP, Branchek TA (2005). . „Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299”. Proceedings of the National Academy of Sciences of the United States of America. 102 (48): 17489—94. PMC 1283534 Слободан приступ. PMID 16287967. doi:10.1073/pnas.0508970102. 

Spoljašnje veze

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