title: Visual and quantitative screening of α1-adrenoceptor antagonists in living cells using quantum dots.
abstract: The performance of α1-adrenoceptor antagonists in living cells was assessed using quantum dots conjugated to a derivative of the α1-adrenoceptor antagonist prazosin. The optimum receptor binding condition and apparent Kd of prazosin-conjugated quantum dots was first determined, followed by application of these structures to drug screening. Total internal reflection fluorescence microscopy and flow cytometry were used to visually and quantitatively measure the affinity of five candidate drugs. The observed affinity order and the affinity coefficient Ki were consistent with previously reported values. These results suggest that this method is suitable for specific drug screening in living cells and is able to realize the displacement assay over the large ranges of dissociation constants.
authors.affiliation: School of Pharmacy, Shandong University , Wenhua Xilu 44, 250012 Jinan, Shandong Province, P. R. China.
authors.forename: Jing
authors.initials: J
authors.lastname: Ma
authors.forename: Zhun
authors.initials: Z
authors.lastname: Hou
authors.forename: Yao
authors.initials: Y
authors.lastname: Song
authors.forename: Lei
authors.initials: L
authors.lastname: Wang
authors.forename: Exiang
authors.initials: E
authors.lastname: Guo
mesh_terms: D058668:Adrenergic alpha-1 Receptor Antagonists / Q000032:analysis* / Q000494:pharmacology*; D002470:Cell Survival; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D057809:HEK293 Cells; D006801:Humans; D011224:Prazosin / Q000032:analysis / Q000494:pharmacology; D045663:Quantum Dots; D018340:Receptors, Adrenergic, alpha-1 / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D058668:Adrenergic alpha-1 Receptor Antagonists; D018340:Receptors, Adrenergic, alpha-1; D011224:Prazosin