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Titolo:
Human 5-hydroxytryptamine(5A) receptors activate coexpressed G(i) and G(o)proteins in Spodoptera frugiperda 9 cells
Autore:
Francken, BJB; Josson, K; Lijnen, P; Jurzak, M; Luyten, WHML; Leysen, JE;
Indirizzi:
Janssen Res Fdn, Dept Biochem Pharmacol, B-2340 Beerse, Belgium Janssen Res Fdn Beerse Belgium B-2340 Pharmacol, B-2340 Beerse, Belgium Janssen Res Fdn, Dept Funct Genom, B-2340 Beerse, Belgium Janssen Res FdnBeerse Belgium B-2340 unct Genom, B-2340 Beerse, Belgium
Titolo Testata:
MOLECULAR PHARMACOLOGY
fascicolo: 5, volume: 57, anno: 2000,
pagine: 1034 - 1044
SICI:
0026-895X(200005)57:5<1034:H5RACG>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
5-HT5A SEROTONIN RECEPTOR; PHOSPHOLIPASE-C ISOZYMES; INFECTED INSECT CELLS; D2 DOPAMINE-RECEPTOR; ALPHA-SUBUNITS; SF9 CELLS; ADENYLATE-CYCLASE; HEK-293 CELLS; RECONSTITUTION; EXPRESSION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
38
Recensione:
Indirizzi per estratti:
Indirizzo: Leysen, JE Janssen Pharmaceut, Turnhoutseweg 30, B-2340 Beerse, Belgium Janssen Pharmaceut Turnhoutseweg 30 Beerse Belgium B-2340 gium
Citazione:
B.J.B. Francken et al., "Human 5-hydroxytryptamine(5A) receptors activate coexpressed G(i) and G(o)proteins in Spodoptera frugiperda 9 cells", MOLEC PHARM, 57(5), 2000, pp. 1034-1044

Abstract

The ability of the human 5-hydroxytryptamine serotonin type 5A (h5-ht(5A))receptor to couple to G proteins from distinct families was investigated through the simultaneous infection of Spodoptera frugiperda 9 insect cells with recombinant baculoviruses encoding the various proteins. Expression of G proteins was demonstrated in immunoblots. Receptor-G protein coupling wasmonitored by high-affinity agonist binding and agonist-induced stimulationof [S-35]guanosine-5'-O-(3-thio) triphosphate binding to membranes. Receptors expressed alone displayed low-affinity agonist binding, and endogenous G proteins were only poorly stimulated on the addition of 5-hydroxytryptamine. When receptors were coexpressed with mammalian G(i)/G(o) proteins (G alpha(i) or G alpha(o) plus G beta(1)gamma(2)), the coupled phenotype was achieved: agonists bound with high affinity in a guanosine-5'-(beta,gamma-imido)triphosphate-sensitive manner and stimulated [S-35]guanosine-5'-O-(3-thio)triphosphate binding to high levels. These effects were not observed on coexpression with G(z)/G(s)/G(q/11/16) or G(12/13). Various ligands were evaluated for their agonistic, antagonistic, or inverse agonistic behavior in both receptor binding and activation assays. Although G(o) displayed different receptor coupling characteristics than G(i) proteins, no clear coupling preference was evident. Coexpression of receptors and G alpha(i) subunits without G beta(1)gamma(2) produced increases in both agonist affinity and maximum G protein activation that were smaller than those in the presence of G beta(1)gamma(2), suggesting that G beta(1)gamma(2) coexpression improves receptor-G protein coupling. Similarly, coexpression of receptors with G beta(1)gamma(2) alone resulted in an improved interaction with endogenous G proteins. Our results demonstrate that h5-ht(5A) receptors expressed in Spodoptera frugiperda 9 cells selectively and functionally couple to coexpressed mammalian G(i) and G(o) proteins.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/20 alle ore 22:02:28