Probing the bradykinin receptor: mapping the geometric topography using ethers of hydroxyproline in novel peptides.
Agents Actions Suppl
; 38 ( Pt 1): 513-25, 1992.
Article
en En
| MEDLINE
| ID: mdl-1334629
ABSTRACT
Five decapeptides were prepared, each having the generic primary sequence D-Arg0-Arg1-Pro2-Hyp3-Gly4-Thi5-Ser6-X7 -Y8-Arg9. A C-terminal beta-turn was anticipated when X was an alkyl ether of D-4-hydroxyproline in either the cis or trans geometric state and Y was either a Tic or Oic residue. Whereas cis ethers have only very weak receptor affinities, the trans ethers are significantly more potent in binding to guinea pig smooth muscle having Ki values as low as 0.16 nM. Notably, these peptides do not contain a D-aromatic amino acid at position 7 of the primary sequence.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Oligopéptidos
/
Receptores de Neurotransmisores
Límite:
Animals
Idioma:
En
Revista:
Agents Actions Suppl
Año:
1992
Tipo del documento:
Article