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Titolo:
DEVELOPMENT OF HIGH-AFFINITY SELECTIVE VIP1 RECEPTOR AGONISTS
Autore:
GOURLET P; VANDERMEERS A; VERTONGEN P; RATHE J; DENEEF P; CNUDDE J; WAELBROECK M; ROBBERECHT P;
Indirizzi:
FREE UNIV BRUSSELS,FAC MED,LAB CHIM BIOL & NUTR,MED SCH,DEPT BIOCHEM & NUTR,BAT G-E,CP 611 B-1070 BRUSSELS BELGIUM FREE UNIV BRUSSELS,FAC MED,LAB CHIM BIOL & NUTR,MED SCH,DEPT BIOCHEM & NUTR B-1070 BRUSSELS BELGIUM
Titolo Testata:
Peptides
fascicolo: 10, volume: 18, anno: 1997,
pagine: 1539 - 1545
SICI:
0196-9781(1997)18:10<1539:DOHSVR>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
PITUITARY ADENYLATE-CYCLASE; VASOACTIVE-INTESTINAL-PEPTIDE; ACTIVATING POLYPEPTIDE PACAP; FUNCTIONAL EXPRESSION; SUP-T1 LYMPHOBLASTS; MOLECULAR-CLONING; CELL-MEMBRANES; FACTOR GRF; SECRETIN; RAT;
Keywords:
VIP SELECTIVE AGONISTS; VIP1 RECEPTOR; VIP2 RECEPTOR; PACAP RECEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
36
Recensione:
Indirizzi per estratti:
Citazione:
P. Gourlet et al., "DEVELOPMENT OF HIGH-AFFINITY SELECTIVE VIP1 RECEPTOR AGONISTS", Peptides, 18(10), 1997, pp. 1539-1545

Abstract

The biological effects of VIP are mediated by at least two VIP receptors: the VIP1 and the VIP2 receptors that were cloned in rat, human and mice. As the mRNA coding for each receptor are located in different tissues, it is likely that each receptor modulates different functions. It is therefore of interest to obtain selective agonists for each receptor subtype. In the present work, we achieved the synthesis of two VIP1 receptor selective agonists derived from secretin and GRF. [R-16]chicken secretin had IC50 values of binding of 1, 10,000, 20, and 3000nM for the rat VIP1, VIP2-, secretin- and PACAP receptors, respectively. This peptide, however, had a weaker affinity for the human VLP1 receptor (IC50 of 60 nM). The chimeric, substituted peptide [K-15,R-16,L-27]VIP(1-7)/GRF(8-27) had IC50 values of binding of 1, 10,000, 10,000and 30,000 nM for the rat VIP1-, VIP2-, secretin- and PACAP receptors. respectively. Furthermore, its also showed an IC50 of 0.8 nM for thehuman VIP1 receptor and a low affinity for the human VIP2 receptor. It is unlikely that this GRF analogue interacted with a high affinity to the pituitary GRF receptors as it did not stimulate rat pituitary adenylate cyclase activity. The two described analogues stimulated maximally the adenylate cyclase activity on membranes expressing each receptor subtype. (C) 1997 Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/03/20 alle ore 15:20:34