| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T10670 | ||||
| Target Name | Neuropeptide Y receptor type 2 (NPY2R) | ||||
| Type of Target |
Clinical trial |
||||
| Drug Potency against Target | PYY3-36 | Drug Info | IC50 = 1.3 nM | [4] | |
| AcNPY(25-36) | Drug Info | Ki = 75 nM | [2] | ||
| AcPYY(22-36) | Drug Info | Ki = 9 nM | [2] | ||
| AcPYY(25-36) | Drug Info | Ki = 30 nM | [2] | ||
| AcPYY(26-36) | Drug Info | Ki = 670 nM | [2] | ||
| Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | Ki = 360 nM | [1] | ||
| H-[Trp-Arg-Nva-Arg-Tyr]2-NH2 | Drug Info | Ki = 1050 nM | [1] | ||
| H-[Trp-Arg-Nva-Arg-Tyr]3-NH2 | Drug Info | Ki = 50 nM | [1] | ||
| LRHYLNLLTRQRY-NH2 | Drug Info | Ki = 5 nM | [3] | ||
| Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | Ki = 310 nM | [1] | ||
| PYY(22-36) | Drug Info | Ki = 3 nM | [2] | ||
| PYY(25-36) | Drug Info | Ki = 270 nM | [2] | ||
| Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | Ki = 390 nM | [1] | ||
| Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2 | Drug Info | Ki = 890 nM | [1] | ||
| Action against Disease Model | PYY3-36 | Drug Info | Pharmacological and genetic approaches have revealed that the Y2-receptor mediates the anorectic effects of PYY3-36 whilst mechanistic studies in rodents identified the hypothalamus, vagus and brainstem regions as potential sites of action. More recently, using functional brain imaging techniques in h uMans, PYY3-36 was found to modulate neuronal activity within hypothalamicand brainstem, and brain regions involved in reward processing | [5] | |
| References | |||||
| REF 1 | Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar a... J Med Chem. 2006 Apr 20;49(8):2661-5. | ||||
| REF 2 | Identification of selective neuropeptide Y2 peptide agonists. Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. | ||||
| REF 3 | A long-acting selective neuropeptide Y2 receptor PEGylated peptide agonist reduces food intake in mice. Bioorg Med Chem Lett. 2007 Apr 1;17(7):1916-9. | ||||
| REF 4 | Gut hormone PYY(3-36) physiologically inhibits food intake. Nature. 2002 Aug 8;418(6898):650-4. | ||||
| REF 5 | The role of peptide YY in appetite regulation and obesity. J Physiol. 2009 Jan 15;587(1):19-25. | ||||
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