| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T39123 | ||||
| Target Name | G-protein coupled receptor 54 | ||||
| Target Type | Discontinued |
||||
| Drug Potency against Target | 4-fluorobenzoyl-Phe-Gly-Leu-Arg-Trp-NH2 | Drug Info | IC50 = 0.71 nM | [529804] | |
| Action against Disease Model | TAK-683 | TAK-683 Hormone regulation on cancer cell line | Drug Info | ||
| The Effect of Target Knockout, Knockdown or Genetic Variations | The ligand for GPR54 has been identified as a peptide derived from the KiSS-1 gene. KiSS-1 has been shown to have anti-metastatic effects, suggesting that KiSS-1 or its receptorrepresents a potential therapeutic target. To further our understanding of the physiological function of this receptor, we have generated a mutant mouse line with a targeted disruption of the GPR54 receptor (GPR54 -/-). The analysis of the GPR54 mutant mice revealed developmental abnormalities of both male and female genitalia and histopathological changes in tissues which normally contain sexually dimorphic features. These data suggest a role for GPR54/KiSS-1 in normal sexual development, and indicate that study of the GPR54 mutant mice may provide valuable insights into h uMan reproductive syndromes | [529804] | |||
| References | |||||
| Ref 529804 | J Med Chem. 2008 Dec 11;51(23):7645-9.Development of novel G-protein-coupled receptor 54 agonists with resistance to degradation by matrix metalloproteinase. | ||||
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