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Peptide YY (PYY), also known as peptide tyrosine tyrosine, is a peptide that in humans is encoded by the PYY gene. Peptide YY is a short peptide released from cells in the ileum and colon in response to feeding. In the blood, gut, and other elements of periphery, PYY acts to reduce appetite; similarly, when injected directly into the central nervous system, PYY is also anorexigenic, i.e., it reduces appetite.
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Neuropeptide Y receptor type 5 is a protein that in humans is encoded by the NPY5R gene.
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Annette Gabriele Beck-Sickinger is a German chemist and biologist. She has been a full professor of Biochemistry and Bioorganic Chemistry at the University of Leipzig since 1999.
Velneperit (S-2367) is a drug developed by Shionogi, which acts as a potent and selective antagonist for the Neuropeptide Y receptor Y5. It has anorectic effects and was developed as a possible treatment for obesity, but was discontinued from further development after disappointing results in Phase II clinical trials. However it was still considered a successful proof of concept of the potential of Y5 receptor antagonists as possible anti-obesity agents in future.
GLP1 poly-agonist peptides are a class of drugs that activate multiple peptide hormone receptors including the glucagon-like peptide-1 (GLP-1) receptor. These drugs are developed for the same indications as GLP-1 receptor agonists—especially obesity, type 2 diabetes, and non-alcoholic fatty liver disease. They are expected to provide superior efficacy with fewer adverse effects compared to GLP-1 mono-agonists, which are dose-limited by gastrointestinal disturbances. The effectiveness of multi-receptor agonists could possibly equal or exceed that of bariatric surgery. The first such drug to receive approval is tirzepatide, a dual agonist of GLP-1 and GIP receptors.
References
- ↑ Michel MC, Beck-Sickinger A, Cox H, Doods HN, Herzog H, Larhammar D, Quirion R, Schwartz T, Westfall T (March 1998). "XVI. International Union of Pharmacology recommendations for the nomenclature of neuropeptide Y, peptide YY, and pancreatic polypeptide receptors". Pharmacol. Rev. 50 (1): 143–50. PMID 9549761.
- ↑ Heilig M (August 2004). "The NPY system in stress, anxiety and depression". Neuropeptides. 38 (4): 213–24. doi:10.1016/j.npep.2004.05.002. PMID 15337373. S2CID 37034137.
- ↑ Harro J (October 2006). "CCK and NPY as anti-anxiety treatment targets: promises, pitfalls, and strategies". Amino Acids. 31 (3): 215–30. doi:10.1007/s00726-006-0334-x. PMID 16738800. S2CID 2017793.
- ↑ Eaton K, Sallee FR, Sah R (2007). "Relevance of neuropeptide Y (NPY) in psychiatry". Current Topics in Medicinal Chemistry. 7 (17): 1645–59. doi:10.2174/156802607782341037. PMID 17979774.
- ↑ Xapelli S, Agasse F, Ferreira R, Silva AP, Malva JO (November 2006). "Neuropeptide Y as an endogenous antiepileptic, neuroprotective and pro-neurogenic peptide". Recent Patents on CNS Drug Discovery. 1 (3): 315–24. doi:10.2174/157488906778773689. PMID 18221213.
- ↑ Vona-Davis LC, McFadden DW (2007). "NPY family of hormones: clinical relevance and potential use in gastrointestinal disease". Current Topics in Medicinal Chemistry. 7 (17): 1710–20. doi:10.2174/156802607782340966. PMID 17979780.
- ↑ Lindner D, Stichel J, Beck-Sickinger AG (September 2008). "Molecular recognition of the NPY hormone family by their receptors". Nutrition (Burbank, Los Angeles County, Calif.). 24 (9): 907–17. doi:10.1016/j.nut.2008.06.025. PMID 18725086.
- ↑ 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 (April 2018). "1 receptor". Nature. 556 (7702): 520–524. doi:10.1038/s41586-018-0046-x. PMC 5920736 . PMID 29670288.
- ↑ Larhammar D, Salaneck E (2004). "Molecular evolution of NPY receptor subtypes". Neuropeptides. 38 (4): 141–51. doi:10.1016/j.npep.2004.06.002. PMID 15337367. S2CID 43696257.
- ↑ Kamiji MM, Inui A (October 2007). "Neuropeptide y receptor selective ligands in the treatment of obesity". Endocrine Reviews. 28 (6): 664–84. doi: 10.1210/er.2007-0003 . PMID 17785427.
- ↑ 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.
- ↑ Kamiji MM, Inui A (2007). "NPY Y2 and Y4 receptors selective ligands: promising anti-obesity drugs?". Current Topics in Medicinal Chemistry. 7 (17): 1734–42. doi:10.2174/156802607782340957. PMID 17979782.
