Characterization of a novel VPAC1selective agonist and identification of the receptor domains implicated in the carboxyl‐terminal peptide recognition
In: British Journal of Pharmacology, Jg. 130 (2000-06-01), Heft 4, S. 819-826
Online
serialPeriodical
Zugriff:
Vasoactive Intestinal Polypeptide (VIP) interacts with a high affinity to two subclasses of G protein coupled receptors named VPAC1and VPAC2, and has a 3–10 fold preference for VPAC1over VPAC2receptors. Selective ligands for each receptor subclass were recently described. [R16]‐PACAP (1–23) and [L22]‐VIP are two selective VPAC1agonists.Chimaeric human VPAC2‐VPAC1recombinant receptors expressed in CHO cells were used to identify the receptor domains implicated in these two selective ligands recognition.The VPAC2preference for [R16]‐PACAP (1–27) over [R16]‐PACAP (1–23) did not require the receptor's NH2‐terminus domain but involved the whole transmembrane domain.In contrast, the selectivity of [L22]‐VIP depended only on the presence of the NH2terminus and EC2domains of the VPAC1receptor.The present data support the idea that in the GPCR‐B family of receptors the different selective ligands require different domains for their selectivity, and that the peptides carboxyl terminal sequence (amino acids 24–27) folds back on the transmembrane receptor domain, close to the peptides, aminoterminus.
Titel: |
Characterization of a novel VPAC1selective agonist and identification of the receptor domains implicated in the carboxyl‐terminal peptide recognition
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Autor/in / Beteiligte Person: | Van Rampelbergh, Jean ; Juarranz, Maria‐Guillerma ; Perret, Jason ; Bondue, Antoine ; Solano, Rosa Maria ; Delporte, Christine ; De Neef, Philippe ; Robberecht, Patrick ; Waelbroeck, Magali |
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Zeitschrift: | British Journal of Pharmacology, Jg. 130 (2000-06-01), Heft 4, S. 819-826 |
Veröffentlichung: | 2000 |
Medientyp: | serialPeriodical |
ISSN: | 0007-1188 (print) ; 1476-5381 (print) |
DOI: | 10.1038/sj.bjp.0703384 |
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