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IR@PKUHSC  > 北京大学第三临床医学院  > 心血管内科  > 期刊论文
学科主题: 临床医学
题名:
Visual and Quantitative Screening of alpha(1)-Adrenoceptor Antagonists in Living Cells Using Quantum Dots
作者: 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
发表日期: 2014-04-01
DOI: 10.1021/co400031s
卷: 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
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
项目资助者: National Natural Science Foundation of China
WOS记录号: WOS:000334571500001
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59994
Appears in Collections:北京大学第三临床医学院_心血管内科_期刊论文

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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:
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.
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