The study of 5-Hydroxytryptamine 2B receptor-nanodisc self-assembling and its ligand binding activity

VernacularTitle:5-羟色胺2B受体Nanodisc自组装及其配体结合活性研究
Author: Shuyan DAI ; Fang PENG ; Jun LI ; Lingzhi QU ; Longying JIANG ; Xiaojuan CHEN ; Ming GUO ; Meiying SHAO ; Yongheng CHEN
Keywords: Receptors,serotonin/CH; Nanocomposites; Receptors,G-protein-coupled; Ligands; Drug evaluation,preclinica
From: Journal of Chinese Physician 2017;19(7):984-987
CountryChina
Language:Chinese
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.