Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UNIPROT:P46098 (
5-HT3 receptor
)
2,290
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Human
serotonin receptor 3A
(
5-HT3A
) is a ligand-gated ion channel regulated by serotonin. A fusion protein (P9-
5-HT3A
) of
5-HT3A
with the P9 protein, a major envelope protein of bacteriophage phi6, was highly expressed in the membrane fraction of Escherichia coli, and the expressed protein was purified to homogeneity using an affinity chromatography. P9-
5-HT3A
was observed as mixed oligomers in detergents. The purified P9-
5-HT3A
was efficiently reconstituted into proteoliposomes, and the serotonin-dependent ion-channel activity of P9-
5-HT3A
was observed by measuring the increased fluorescence of
Fluo-3
attributed to the formation of a complex with the Ca(2+) ions released from the proteoliposomes. Alanine substitution for Trp178 of
5-HT3A
abolished the serotonin-dependent ion-channel activity, confirming the importance of Trp178 as a ligand-binding site. Furthermore, the ion-channel activity of the reconstituted P9-
5-HT3A
was effectively blocked by treatment with ondansetron, an antagonist of
5-HT3A
. The bacterial expression system of human
5-HT3A
and the proteoliposomes reconstituted with
5-HT3A
would provide biophysical and structural analyses of
5-HT3A
.
...
PMID:Bacterially expressed human serotonin receptor 3A is functionally reconstituted in proteoliposomes. 2332 Oct 66
