The study of 5-Hydroxytryptamine 2B receptor-nanodisc self-assembling and its ligand binding activity / 中国医师杂志
Journal of Chinese Physician
;
(12): 984-987, 2017.
Artigo
em Chinês
| WPRIM
| ID: wpr-613278
ABSTRACT
Objective To explore the application of nanodisc in functional and drug discovery research of G protein-coupled receptor (GPCR).Methods The purified recombinant 5-Hydroxytryptamine 2B receptor (5-HT2BR) was reconstituted into nanodisc complex.Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) and size exclution chromatography were performed to evaluate the reconstitution reaction,followed by the use of surface plasmon resonance to validate the ligand-binding activity of 5-HT2BR after reconstitution.Results 5-HT2B R was effectively self-assembled into nanodisc while maintained its binding activity toward the antagonist SB204741.Conclusions The presented study provided potential application of 5-HT2B R-nanodisc for the development of subtype-selective drugs against 5-HT2B R and the fundamental of utilizing nanodisc for GPCR structural and functional studies as well as drug discovery.
Texto completo:
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Índice:
WPRIM (Pacífico Ocidental)
Idioma:
Chinês
Revista:
Journal of Chinese Physician
Ano de publicação:
2017
Tipo de documento:
Artigo
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