Neuropeptide Y receptor Y1 explained

Neuropeptide Y receptor type 1 is a protein that in humans is encoded by the NPY1R gene.^{[1] [2]}

Selective ligands

Agonists

• Neuropeptide Y (endogenous agonist, non subtype selective)
• Peptide YY

Antagonists

Peptide

• BVD-10 (selective NPY₁ antagonist, CAS# 262418-00-8)
• GR-231,118 (mixed NPY₁ antagonist / NPY₄ agonist, CAS# 158859-98-4)

Non-peptide

• BIBO-3304 (CAS# 191868-14-1)
• BIBP-3226 (CAS# 159013-54-4)
• PD-160,170 (CAS# 181468-88-2)

Available Structures

• 5ZBH (Neuropeptide Y1 bound to antagonist BMS-193835)^[3]
• 5ZBQ (Neuropeptide Y1 bound to antagonist UR-MK299)

See also

• Neuropeptide Y receptor

Further reading

• Wan CP, Lau BH . Neuropeptide Y receptor subtypes . Life Sciences . 56 . 13 . 1055–64 . February 1995 . 9001438 . 10.1016/0024-3205(95)00041-4 .
• Parker E, Van Heek M, Stamford A . Neuropeptide Y receptors as targets for anti-obesity drug development: perspective and current status . European Journal of Pharmacology . 440 . 2–3 . 173–87 . April 2002 . 12007534 . 10.1016/S0014-2999(02)01427-9 .
• Bettio A, Beck-Sickinger AG . Biophysical methods to study ligand-receptor interactions of neuropeptide Y . Biopolymers . 60 . 6 . 420–37 . 2002 . 12209475 . 10.1002/1097-0282(2001)60:6<420::AID-BIP10183>3.0.CO;2-W .
• Larhammar D, Blomqvist AG, Yee F, Jazin E, Yoo H, Wahlested C . Cloning and functional expression of a human neuropeptide Y/peptide YY receptor of the Y1 type . The Journal of Biological Chemistry . 267 . 16 . 10935–8 . June 1992 . 10.1016/S0021-9258(19)49854-2 . 1317848 . free .
• Herzog H, Hort YJ, Ball HJ, Hayes G, Shine J, Selbie LA . Cloned human neuropeptide Y receptor couples to two different second messenger systems . Proceedings of the National Academy of Sciences of the United States of America . 89 . 13 . 5794–8 . July 1992 . 1321422 . 402104 . 10.1073/pnas.89.13.5794 . 1992PNAS...89.5794H . free .
• Rose PM, Fernandes P, Lynch JS, Frazier ST, Fisher SM, Kodukula K, Kienzle B, Seethala R . Cloning and functional expression of a cDNA encoding a human type 2 neuropeptide Y receptor . The Journal of Biological Chemistry . 270 . 39 . 22661–4 . September 1995 . 7559383 . 10.1074/jbc.270.39.22661 . free .
• Gicquiaux H, Lecat S, Gaire M, Dieterlen A, Mély Y, Takeda K, Bucher B, Galzi JL . Rapid internalization and recycling of the human neuropeptide Y Y(1) receptor . The Journal of Biological Chemistry . 277 . 8 . 6645–55 . February 2002 . 11741903 . 10.1074/jbc.M107224200 . free .
• Sheriff S, F Qureshy A, T Chance W, Kasckow JW, Balasubramaniam A . Predominant role by CaM kinase in NPY Y(1) receptor signaling: involvement of CREB [corrected] . Peptides . 23 . 1 . 87–96 . January 2002 . 11814622 . 10.1016/S0196-9781(01)00583-6 . 54419749 .
• Cox HM, Tough IR . Neuropeptide Y, Y1, Y2 and Y4 receptors mediate Y agonist responses in isolated human colon mucosa . British Journal of Pharmacology . 135 . 6 . 1505–12 . March 2002 . 11906964 . 1573267 . 10.1038/sj.bjp.0704604 .
• Uddman R, Möller S, Nilsson T, Nyström S, Ekstrand J, Edvinsson L . Neuropeptide Y Y1 and neuropeptide Y Y2 receptors in human cardiovascular tissues . Peptides . 23 . 5 . 927–34 . May 2002 . 12084524 . 10.1016/S0196-9781(02)00003-7 . 31244551 .
• Cantó Soler MV, Gallo JE, Dodds RA, Hökfelt T, Villar MJ, Suburo AM . Y1 receptor of neuropeptide Y as a glial marker in proliferative vitreoretinopathy and diseased human retina . Glia . 39 . 3 . 320–4 . September 2002 . 12203398 . 10.1002/glia.10107 . 41750584 .
• Berglund MM, Schober DA, Statnick MA, McDonald PH, Gehlert DR . The use of bioluminescence resonance energy transfer 2 to study neuropeptide Y receptor agonist-induced beta-arrestin 2 interaction . The Journal of Pharmacology and Experimental Therapeutics . 306 . 1 . 147–56 . July 2003 . 12665544 . 10.1124/jpet.103.051227 . 40163065 .
• Lehner B, Sanderson CM . A protein interaction framework for human mRNA degradation . Genome Research . 14 . 7 . 1315–23 . July 2004 . 15231747 . 442147 . 10.1101/gr.2122004 .
• Körner M, Waser B, Reubi JC . High expression of neuropeptide y receptors in tumors of the human adrenal gland and extra-adrenal paraganglia . Clinical Cancer Research . 10 . 24 . 8426–33 . December 2004 . 15623622 . 10.1158/1078-0432.CCR-04-0821 . free .

External links

• Web site: Neuropeptide Y Receptors: Y₁ . IUPHAR Database of Receptors and Ion Channels . International Union of Basic and Clinical Pharmacology . 2008-12-09 . 2016-03-03 . https://web.archive.org/web/20160303212224/http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2366 . dead .

Notes and References

1. Herzog H, Baumgartner M, Vivero C, Selbie LA, Auer B, Shine J . Genomic organization, localization, and allelic differences in the gene for the human neuropeptide Y Y1 receptor . The Journal of Biological Chemistry . 268 . 9 . 6703–7 . March 1993 . 10.1016/S0021-9258(18)53306-8 . 8095935 . free .
2. Web site: Entrez Gene: NPY1R neuropeptide Y receptor Y1.
3. Yang Z, Han S, Keller M, Kaiser A, Bender BJ, Bosse M, Burkert K, Kögler LM, Wifling D, Bernhardt G, Plank N, Littmann T, Schmidt P, Yi C, Li B, Ye S, Zhang R, Xu B, Larhammar D, Stevens RC, Huster D, Meiler J, Zhao Q, Beck-Sickinger AG, Buschauer A, Wu B . 1 receptor . En . Nature . 556 . 7702 . 520–524 . April 2018 . 29670288 . 5920736 . 10.1038/s41586-018-0046-x .