| Autor: |
R A, Adan, J, Oosterom, R F, Toonen, M V, Kraan, J P, Burbach, W H, Gispen |
| Rok vydání: |
1997 |
| Předmět: |
|
| Zdroj: |
Receptorschannels. 5(3-4) |
| ISSN: |
1060-6823 |
| Popis: |
The cloning of melanocortin receptors opened new avenues to identify selective ligands for this receptor family. gamma-MSH was characterized as a melanocortin-3 receptor selective agonist, [D-Arg8]ACTH-(4-10) and [Pro8,10, Gly9]ACTH-(4-10) were characterized as melanocortin-4 receptor antagonists. The application of these ligands in vivo revealed that melanocortin-4 receptors mediate melanocortin-induced grooming behaviour in the rat. Since we still lack potent and selective melanocortin receptor ligands, we performed homology modelling and site directed mutagenesis of the melanocortin-4 receptor, in order to understand how melanocortins bind melanocortin receptors. A histidine at position 260 in the melanocortin-4 receptor is important for normal receptor function. However this residue is not forming a salt bridge with a glutamate at position 92 to keep the receptor in an inactive conformation, nor with the glutamate in the melanocortin peptides as had been suggested before. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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