IR@PKUHSC  > 北京大学第三临床医学院  > 心血管内科
学科主题临床医学
Visual and Quantitative Screening of alpha(1)-Adrenoceptor Antagonists in Living Cells Using Quantum Dots
Ma, Jing1; Hou, Zhun1; Song, Yao3; Wang, Lei1; Guo, Exiang2
关键词drug screening quantum dots alpha(1)-radrenoceptor antagonist living cells
刊名ACS COMBINATORIAL SCIENCE
2014-04-01
DOI10.1021/co400031s
16期:4页:155-159
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Applied ; Chemistry, Medicinal ; Chemistry, Multidisciplinary
资助者National Natural Science Foundation of China ; National Natural Science Foundation of China
研究领域[WOS]Chemistry ; Pharmacology & Pharmacy
关键词[WOS]PROTEIN-COUPLED RECEPTORS ; BINDING ASSAY ; LIGAND ; ADRENOCEPTOR ; DISCOVERY ; DYNAMICS ; TRACKING ; TARGETS ; SURFACE ; CANCER
英文摘要

The performance of alpha(1)-adrenoceptor antagonists in living cells was assessed using quantum dots conjugated to a derivative of the alpha(1)-adrenoceptor antagonist prazosin. The optimum receptor binding condition and apparent K-d 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 K-i 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.

语种英语
所属项目编号21175082 ; 21175081 ; 20875056
资助者National Natural Science Foundation of China ; National Natural Science Foundation of China
WOS记录号WOS:000334571500001
Citation statistics
Cited Times:3[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/59994
Collection北京大学第三临床医学院_心血管内科
作者单位1.Qingdao Municipal Hosp, Qingdao 266071, Shandong, Peoples R China
2.Shandong Univ, Sch Pharm, Jinan 250012, Shandong, Peoples R China
3.Peking Univ, Hosp 3, Inst Vasc Med, Beijing 100191, Peoples R China
Recommended Citation
GB/T 7714
Ma, Jing,Hou, Zhun,Song, Yao,et al. Visual and Quantitative Screening of alpha(1)-Adrenoceptor Antagonists in Living Cells Using Quantum Dots[J]. ACS COMBINATORIAL SCIENCE,2014,16(4):155-159.
APA Ma, Jing,Hou, Zhun,Song, Yao,Wang, Lei,&Guo, Exiang.(2014).Visual and Quantitative Screening of alpha(1)-Adrenoceptor Antagonists in Living Cells Using Quantum Dots.ACS COMBINATORIAL SCIENCE,16(4),155-159.
MLA Ma, Jing,et al."Visual and Quantitative Screening of alpha(1)-Adrenoceptor Antagonists in Living Cells Using Quantum Dots".ACS COMBINATORIAL SCIENCE 16.4(2014):155-159.
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