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Titolo:
AGONIST AND ANTAGONIST MODULATION OF [S-35] GTP-GAMMA-S BINDING IN TRANSFECTED CHO CELLS EXPRESSING THE NEUROTENSIN RECEPTOR
Autore:
HERMANS E; GEURTS M; MALOTEAUX JM;
Indirizzi:
UNIV LEICESTER,DEPT CELL PHYSIOL & PHARMACOL,MAURICE SHOCK MED SCI BLDG,UNIV RD,POB 138 LEICESTER LE1 9HN LEICS ENGLAND UNIV CATHOLIQUE LOUVAIN,PHARMACOL LAB B-1200 BRUSSELS BELGIUM
Titolo Testata:
British Journal of Pharmacology
fascicolo: 8, volume: 121, anno: 1997,
pagine: 1817 - 1823
SICI:
0007-1188(1997)121:8<1817:AAAMO[>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
HAMSTER OVARY CELLS; GUINEA-PIG BRAIN; G-PROTEINS; GUANOSINE-5'-O-(3-)S-35>THIO)TRIPHOSPHATE BINDING; REGULATORY PROTEINS; SIGNAL-TRANSDUCTION; CARDIAC MEMBRANES; PLASMA-MEMBRANES; SMOOTH-MUSCLE; C ACTIVATION;
Keywords:
NEUROTENSIN; SR-48692; U-73122; [S-35] GTP-GAMMA-S; G-PROTEIN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
50
Recensione:
Indirizzi per estratti:
Citazione:
E. Hermans et al., "AGONIST AND ANTAGONIST MODULATION OF [S-35] GTP-GAMMA-S BINDING IN TRANSFECTED CHO CELLS EXPRESSING THE NEUROTENSIN RECEPTOR", British Journal of Pharmacology, 121(8), 1997, pp. 1817-1823

Abstract

1 The functional interaction of the cloned rat neurotensin receptor with intracellular G-proteins was investigated by studying the binding of the radiolabelled guanylyl nucleotide analogue [S-35]-GTP gamma S induced by neurotensin to membranes prepared from transfected Chinese hamster ovary (CHO) cells. 2 The agonist-induced binding of [S-35]-GTP gamma S was only detected in the presence of NaCl in the incubation buffer. However, it was also demonstrated that the binding of [H-3]-neurotensin to its receptor was inhibited by NaCl. In the presence of 50 mM NaCl, the binding of the labelled nucleotide was about 2 fold increased by stimulation with saturating concentrations of neurotensin (EC50value of 2.3 +/- 0.9 nM). 3 The stimulation of [S-35]-GTP gamma S binding by neurotensin was mimicked by the stable analogue of neurotensin, JMV-449 (EC50 value of 1.7 +/- 0.4 nM) and the neurotensin related peptide neuromedin N (EC50 value of 21 +/- 6 nM). 4 The NT-induced [S-35]-GTP gamma S binding was competitively inhibited by SR48692 (pA(2) value of 9.55 +/- 0.28), a non-peptide neurotensin receptor antagonist. SR48692 alone had no effect on the specific binding of [S-35]-GTP gamma S. 5 The response to neurotensin was found to be inhibited by the aminosteroid U-73122, a putative inhibitor of phospholipase C-dependentprocesses, indicating that this drug may act at the G-protein level. 6 Taken together, these results constitute the first characterization of the exchange of guanylyl nucleotides at the G-protein level that isinduced by the neuropeptide neurotensin after binding to its receptor.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/07/20 alle ore 08:05:13