Neuropeptide Y receptor Y5

Neuropeptide Y receptor Y5
Available structures
PDB	Ortholog search: PDBe, RCSB
List of PDB id codes
	2HE6
Identifiers
Symbols	NPY5R; NPY5-R; NPYR5; NPYY5-R
External IDs	OMIM: 602001 MGI: 108082 HomoloGene: 21241 IUPHAR: Y5 ChEMBL: 4561 GeneCards: NPY5R Gene
Gene Ontology
Molecular function	• peptide YY receptor activity; • pancreatic polypeptide receptor activity; • neuropeptide Y receptor activity;
Cellular component	• cytoplasm; • plasma membrane; • integral to plasma membrane;
Biological process	• positive regulation of acute inflammatory response; • outflow tract morphogenesis; • cardiac left ventricle morphogenesis; • G-protein coupled receptor signaling pathway; • negative regulation of glutamate secretion; • negative regulation of synaptic transmission, GABAergic; • eating behavior; • positive regulation of smooth muscle cell proliferation; • generation of ovulation cycle rhythm;
	Sources: Amigo / QuickGO
RNA expression pattern
	More reference expression data
Orthologs
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Neuropeptide Y receptor type 5 is a protein that in humans is encoded by the NPY5R gene.¹²³

Selective Ligands

Agonists

Neuropeptide Y (endogenous agonist, non subtype selective)
BWX-46 (selective NPY₅ agonist, CAS# 172997-92-1)
Peptide YY

Antagonists

CGP-71683 (CAS# 192322-50-2)
FMS-586⁴
L-152,804 (CAS# 6508-43-6)
Lu AA-33810⁵
MK-0557⁶
NTNCB (CAS# 486453-65-0)⁷

References

^ Gerald C, Walker MW, Criscione L, Gustafson EL, Batzl-Hartmann C, Smith KE, Vaysse P, Durkin MM, Laz TM, Linemeyer DL, Schaffhauser AO, Whitebread S, Hofbauer KG, Taber RI, Branchek TA, Weinshank RL (Aug 1996). "A receptor subtype involved in neuropeptide-Y-induced food intake". Nature 382 (6587): 168–71. doi:10.1038/382168a0. PMID 8700207.
^ Lutz CM, Richards JE, Scott KL, Sinha S, Yang-Feng TL, Frankel WN, Thompson DA (Feb 1998). "Neuropeptide Y receptor genes mapped in human and mouse: receptors with high affinity for pancreatic polypeptide are not clustered with receptors specific for neuropeptide Y and peptide YY". Genomics 46 (2): 287–90. doi:10.1006/geno.1997.5024. PMID 9417917.
^ "Entrez Gene: NPY5R neuropeptide Y receptor Y5".
^ Kakui N, Tanaka J, Tabata Y, Asai K, Masuda N, Miyara T, Nakatani Y, Ohsawa F, Nishikawa N, Sugai M, Suzuki M, Aoki K, Kitaguchi H (May 2006). "Pharmacological characterization and feeding-suppressive property of FMS586 [3-(5,6,7,8-tetrahydro-9-isopropyl-carbazol-3-yl)-1-methyl-1-(2-pyridin-4-yl-ethyl)-urea hydrochloride], a novel, selective, and orally active antagonist for neuropeptide Y Y5 receptor". The Journal of Pharmacology and Experimental Therapeutics 317 (2): 562–70. doi:10.1124/jpet.105.099705. PMID 16436501.
^ Walker MW, Wolinsky TD, Jubian V, Chandrasena G, Zhong H, Huang X, Miller S, Hegde LG, Marsteller DA, Marzabadi MR, Papp M, Overstreet DH, Gerald CP, Craig DA (March 2009). "The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 (N-([trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl)-methanesulfonamide) exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity". The Journal of Pharmacology and Experimental Therapeutics 328 (3): 900–11. doi:10.1124/jpet.108.144634. PMID 19098165.
^ MacNeil DJ (2007). "NPY Y1 and Y5 receptor selective antagonists as anti-obesity drugs". Current Topics in Medicinal Chemistry 7 (17): 1721–33. doi:10.2174/156802607782341028. PMID 17979781.
^ Islam I, Dhanoa D, Finn J, Du P, Walker MW, Salon JA, Zhang J, Gluchowski C (July 2002). "Discovery of potent and selective small molecule NPY Y5 receptor antagonists". Bioorganic & Medicinal Chemistry Letters 12 (13): 1767–9. doi:10.1016/S0960-894X(02)00287-1. PMID 12067557.

External links

"Neuropeptide Y Receptors: Y₅". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.

Parker E, Van Heek M, Stamford A (2002). "Neuropeptide Y receptors as targets for anti-obesity drug development: perspective and current status.". Eur. J. Pharmacol. 440 (2–3): 173–87. doi:10.1016/S0014-2999(02)01427-9. PMID 12007534.
Hu Y, Bloomquist BT, Cornfield LJ, et al. (1996). "Identification of a novel hypothalamic neuropeptide Y receptor associated with feeding behavior". J. Biol. Chem. 271 (42): 26315–9. doi:10.1074/jbc.271.42.26315. PMID 8824284.
Herzog H, Darby K, Ball H, et al. (1997). "Overlapping gene structure of the human neuropeptide Y receptor subtypes Y1 and Y5 suggests coordinate transcriptional regulation". Genomics 41 (3): 315–9. doi:10.1006/geno.1997.4684. PMID 9169127.
Nichol KA, Morey A, Couzens MH, et al. (1999). "Conservation of expression of neuropeptide Y5 receptor between human and rat hypothalamus and limbic regions suggests an integral role in central neuroendocrine control". J. Neurosci. 19 (23): 10295–304. PMID 10575027.
Rodriguez M, Audinot V, Dromaint S, et al. (2003). "Molecular identification of the long isoform of the human neuropeptide Y Y5 receptor and pharmacological comparison with the short Y5 receptor isoform". Biochem. J. 369 (Pt 3): 667–73. doi:10.1042/BJ20020739. PMC 1223119. PMID 12398768.
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.
Berglund MM, Schober DA, Statnick MA, et al. (2003). "The use of bioluminescence resonance energy transfer 2 to study neuropeptide Y receptor agonist-induced beta-arrestin 2 interaction". J. Pharmacol. Exp. Ther. 306 (1): 147–56. doi:10.1124/jpet.103.051227. PMID 12665544.
Beauverger P, Rodriguez M, Nicolas JP, et al. (2005). "Functional characterization of human neuropeptide Y receptor subtype five specific antagonists using a luciferase reporter gene assay". Cell. Signal. 17 (4): 489–96. doi:10.1016/j.cellsig.2004.09.006. PMID 15601626.
Movafagh S, Hobson JP, Spiegel S, et al. (2006). "Neuropeptide Y induces migration, proliferation, and tube formation of endothelial cells bimodally via Y1, Y2, and Y5 receptors". FASEB J. 20 (11): 1924–6. doi:10.1096/fj.05-4770fje. PMID 16891622.
Coletta DK, Schneider J, Stern MP, et al. (2007). "Association of neuropeptide Y receptor Y5 polymorphisms with dyslipidemia in Mexican Americans". Obesity (Silver Spring, Md.) 15 (4): 809–15. doi:10.1038/oby.2007.610. PMID 17426313.

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[pmid8700207-1] Gerald C, Walker MW, Criscione L, Gustafson EL, Batzl-Hartmann C, Smith KE, Vaysse P, Durkin MM, Laz TM, Linemeyer DL, Schaffhauser AO, Whitebread S, Hofbauer KG, Taber RI, Branchek TA, Weinshank RL (Aug 1996). "A receptor subtype involved in neuropeptide-Y-induced food intake". Nature 382 (6587): 168–71. doi:10.1038/382168a0. PMID 8700207.

[pmid9417917-2] Lutz CM, Richards JE, Scott KL, Sinha S, Yang-Feng TL, Frankel WN, Thompson DA (Feb 1998). "Neuropeptide Y receptor genes mapped in human and mouse: receptors with high affinity for pancreatic polypeptide are not clustered with receptors specific for neuropeptide Y and peptide YY". Genomics 46 (2): 287–90. doi:10.1006/geno.1997.5024. PMID 9417917.

[entrez-3] "Entrez Gene: NPY5R neuropeptide Y receptor Y5".

[pmid16436501-4] Kakui N, Tanaka J, Tabata Y, Asai K, Masuda N, Miyara T, Nakatani Y, Ohsawa F, Nishikawa N, Sugai M, Suzuki M, Aoki K, Kitaguchi H (May 2006). "Pharmacological characterization and feeding-suppressive property of FMS586 [3-(5,6,7,8-tetrahydro-9-isopropyl-carbazol-3-yl)-1-methyl-1-(2-pyridin-4-yl-ethyl)-urea hydrochloride], a novel, selective, and orally active antagonist for neuropeptide Y Y5 receptor". The Journal of Pharmacology and Experimental Therapeutics 317 (2): 562–70. doi:10.1124/jpet.105.099705. PMID 16436501.

[pmid19098165-5] Walker MW, Wolinsky TD, Jubian V, Chandrasena G, Zhong H, Huang X, Miller S, Hegde LG, Marsteller DA, Marzabadi MR, Papp M, Overstreet DH, Gerald CP, Craig DA (March 2009). "The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 (N-([trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl)-methanesulfonamide) exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity". The Journal of Pharmacology and Experimental Therapeutics 328 (3): 900–11. doi:10.1124/jpet.108.144634. PMID 19098165.

[pmid17979781-6] MacNeil DJ (2007). "NPY Y1 and Y5 receptor selective antagonists as anti-obesity drugs". Current Topics in Medicinal Chemistry 7 (17): 1721–33. doi:10.2174/156802607782341028. PMID 17979781.

[pmid12067557-7] Islam I, Dhanoa D, Finn J, Du P, Walker MW, Salon JA, Zhang J, Gluchowski C (July 2002). "Discovery of potent and selective small molecule NPY Y5 receptor antagonists". Bioorganic & Medicinal Chemistry Letters 12 (13): 1767–9. doi:10.1016/S0960-894X(02)00287-1. PMID 12067557.

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Neuropeptide Y receptor Y5

Contents

Selective Ligands

Agonists

Antagonists

See also

References

External links

Further reading