Design and synthesis of potent cystine-free cyclic hexapeptide agonists at the human urotensin receptor.
Org Lett
; 8(9): 1799-802, 2006 Apr 27.
Article
en En
| MEDLINE
| ID: mdl-16623554
ABSTRACT
[structure see text] Cyclic hexapeptides, incorporating a dipeptide unit in place of the disulfide bond found in urotensin, were prepared and screened at the human urotensin receptor. The bridging dipeptide unit was found to influence dramatically the affinity for the urotensin receptor. Alanyl-N-methylalanyl and alanylprolyl dipeptide bridges failed to afford active ligands, while the alanyl-alanyl unit yielded a ligand with submicromolar affinity for the urotensin receptor. Further development led to a hexapeptide agonist with nanomolar affinity (2.8 nM).
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Banco de datos:
MEDLINE
Asunto principal:
Péptidos Cíclicos
/
Urotensinas
/
Receptores Acoplados a Proteínas G
/
Dipéptidos
Límite:
Humans
Idioma:
En
Revista:
Org Lett
Asunto de la revista:
BIOQUIMICA
Año:
2006
Tipo del documento:
Article
País de afiliación:
Estados Unidos