Biology:Galanin receptor

From HandWiki
Short description: InterPro Family
galanin receptor 1
Identifiers
SymbolGALR1
Alt. symbolsGALNR1, GALNR
NCBI gene2587
HGNC4132
OMIM600377
RefSeqNM_001480
UniProtP47211
Other data
LocusChr. 18 q23
galanin receptor 2
Identifiers
SymbolGALR2
NCBI gene8811
HGNC4133
OMIM603691
RefSeqNM_003857
UniProtO43603
Other data
LocusChr. 17 q25.3
galanin receptor 3
Identifiers
SymbolGALR3
NCBI gene8484
HGNC4134
OMIM603692
RefSeqNM_003614
UniProtO60755
Other data
LocusChr. 22 q12.2-13.1

The galanin receptor is a G protein-coupled receptor, or metabotropic receptor which binds galanin.[1]

Galanin receptors can be found throughout the peripheral and central nervous systems and the endocrine system. So far three subtypes are known to exist: GAL-R1, GAL-R2, and GAL-R3.[2] The specific function of each subtype remains to be fully elucidated, although as of 2009 great progress is currently being made in this respect with the generation of receptor subtype-specific knockout mice,[3][4] and the first selective ligands for galanin receptor subtypes. Selective galanin agonists are anticonvulsant,[5][6][7] while antagonists produce antidepressant and anxiolytic effects in animals,[8][9][10][11][12] so either agonist or antagonist ligands for the galanin receptors may be potentially therapeutic compounds in humans.

Ligands

Agonists

Non-selective
GAL1 selective
GAL1/2 selective
  • M1154 - has no GalR3 interaction[19]
GAL2 selective
  • Galanin 2-11 amide - also called AR-M 1896, anticonvulsant in mice, CAS# 367518-31-8
  • M1145 - selective compared to both GalR1 and GalR3 [20]
  • M1153 - selective compared to both GalR1 and GalR3[21]
  • CYM 2503 (positive allosteric modulator)[22]

Antagonists

Non-selective
  • M35 peptide
GAL1 selective
GAL2 selective
GAL3 selective

References

  1. ↑ "The galanin peptide family: receptor pharmacology, pleiotropic biological actions, and implications in health and disease". Pharmacol. Ther. 115 (2): 177–207. 2007. doi:10.1016/j.pharmthera.2007.05.009. PMID 17604107. 
  2. ↑ "Galanin receptor subtypes". Trends Pharmacol. Sci. 21 (3): 109–17. 2000. doi:10.1016/S0165-6147(00)01446-2. PMID 10689365. 
  3. ↑ "Galanin impairs performance on learning and memory tasks: findings from galanin transgenic and GAL-R1 knockout mice". Neuropeptides 39 (3): 239–43. June 2005. doi:10.1016/j.npep.2004.12.026. PMID 15944016. https://zenodo.org/record/1259271. 
  4. ↑ "Phenotypic analysis of GalR2 knockout mice in anxiety- and depression-related behavioral tests". Neuropeptides 42 (4): 387–97. August 2008. doi:10.1016/j.npep.2008.04.009. PMID 18554714. 
  5. ↑ "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. August 2006. doi:10.1124/jpet.106.104703. PMID 16699066. 
  6. ↑ "Galanin and epilepsy". Cellular and Molecular Life Sciences 65 (12): 1864–71. June 2008. doi:10.1007/s00018-008-8161-8. PMID 18500639. 
  7. ↑ "Structural Requirements for a Lipoamino Acid in Modulating the Anticonvulsant Activities of Systemically Active Galanin Analogues". Journal of Medicinal Chemistry 52 (5): 1310–6. February 2009. doi:10.1021/jm801397w. PMID 19199479. 
  8. ↑ "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. January 2005. doi:10.1073/pnas.0408891102. PMID 15647369. Bibcode: 2005PNAS..102..874L. 
  9. ↑ "A novel, systemically active, selective galanin receptor type-3 ligand exhibits antidepressant-like activity in preclinical tests". Neuroscience Letters 405 (1–2): 111–5. September 2006. doi:10.1016/j.neulet.2006.06.033. PMID 16854525. 
  10. ↑ "The brain galanin receptors: targets for novel antidepressant drugs". CNS & Neurological Disorders Drug Targets 6 (3): 183–92. June 2007. doi:10.2174/187152707780619335. PMID 17511615. 
  11. ↑ "Galanin, galanin receptor subtypes and depression-like behaviour". Cellular and Molecular Life Sciences 65 (12): 1854–63. June 2008. doi:10.1007/s00018-008-8160-9. PMID 18500640. 
  12. ↑ "Differential role of galanin receptors in the regulation of depression-like behavior and monoamine/stress-related genes at the cell body level". Neuropsychopharmacology 33 (11): 2573–85. October 2008. doi:10.1038/sj.npp.1301660. PMID 18172432. 
  13. ↑ "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. November 2004. doi:10.1073/pnas.0407543101. PMID 15557002. Bibcode: 2004PNAS..10116727C. 
  14. ↑ "Anxiolytic-like activity of the non-selective galanin receptor agonist, galnon". Neuropeptides 41 (5): 307–20. October 2007. doi:10.1016/j.npep.2007.05.001. PMID 17637475. 
  15. ↑ "Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities". Journal of Medicinal Chemistry 51 (24): 8038–47. December 2008. doi:10.1021/jm801088x. PMID 19053761. 
  16. ↑ "Developing novel antiepileptic drugs: characterization of NAX 5055, a systemically-active galanin analog, in epilepsy models". Neurotherapeutics 6 (2): 372–80. April 2009. doi:10.1016/j.nurt.2009.01.001. PMID 19332332. 
  17. ↑ Robertson, CR (May 2012). "Generating orally active galanin analogues with analgesic activities". ChemMedChem 7 (5): 903–9. doi:10.1002/cmdc.201100574. PMID 22374865. 
  18. ↑ 18.0 18.1 "Binding of Chimeric Peptides M617 and M871 to Galanin Receptor Type 3 Reveals Characteristics of Galanin Receptor–Ligand Interaction". International Journal of Peptide Research and Therapeutics 16 (1): 17–22. March 2010. doi:10.1007/s10989-009-9197-9. 
  19. ↑ "M1154 – A Novel Galanin Ligand to Delineate the Galaninergic System". Proceedings of the 31st European Peptide Symposium: 452–453. 2010. http://www.eurpepsoc.com/details/features/881017/Proceedings_of_the_31st_European_Peptide_Symposium.html. 
  20. ↑ "A novel GalR2-specific peptide agonist". Neuropeptides 43 (3): 187–92. 2009. doi:10.1016/j.npep.2009.04.004. PMID 19467704. 
  21. ↑ "Novel galanin receptor subtype specific ligands in feeding regulation". Neurochemistry International 58 (6): 714–720. 2011. doi:10.1016/j.neuint.2011.02.012. PMID 21333705. 
  22. ↑ Mittapalli, GK (2014). "Structure Activity Relationships of Novel Antiepileptic Drugs". Curr Med Chem 21 (6): 722–54. doi:10.2174/0929867320666131119153215. PMID 24251563. 
  23. ↑ "Galanin receptor antagonists : a potential novel pharmacological treatment for mood disorders". CNS Drugs 20 (8): 633–54. 2006. doi:10.2165/00023210-200620080-00003. PMID 16863269. 
  24. ↑ "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. November 2005. doi:10.1073/pnas.0508970102. PMID 16287967. Bibcode: 2005PNAS..10217489S. 
  25. ↑ "Theoretical investigation of selective ligand binding mode of galanin receptors". Journal of Biomolecular Structure and Dynamics 40 (23): 12964–12974. October 2021. doi:10.1080/07391102.2021.1977703. PMID 34632940. https://figshare.com/articles/journal_contribution/16782946. 

External links



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