Identification of upregulators of human ATP-binding cassette transporter A1 via high-throughput screening of a synthetic and natural compound library [0.03%]
人ATP结合盒转运蛋白A1上调诱导剂的筛选及鉴定：全自动化高通量筛选合成及天然化合物文库
Jie Gao,Yanni Xu,Yuan Yang et al.
Jie Gao et al.
The ATP-binding cassette transporter A1 (ABCA1) is a membrane transporter that directly contributes to high-density lipoprotein (HDL) biogenesis by mediating the cellular efflux of cholesterol and phospholipids to lipid-poor apolipoprotein ...
Development of an HTS assay for the search of anti-influenza agents targeting the interaction of viral RNA with the NS1 protein [0.03%]
抗流感药物高通量筛选体系的建立及初步应用
Marta Maroto,Yolanda Fernandez,Juan Ortin et al.
Marta Maroto et al.
The NS1 protein is a nonstructural protein encoded by the influenza A virus. It is responsible for many alterations produced in the cellular metabolism upon infection by the virus and for modulation of virus virulence. The NS1 protein is ab...
A cell-based PDE4 assay in 1536-well plate format for high-throughput screening [0.03%]
一种基于细胞的PDE4测定法在1536孔板格式中的高通量筛选方法
Steven A Titus,Xiao Li,Noel Southall et al.
Steven A Titus et al.
The cyclic nucleotide phosphodiesterases (PDEs) are intracellular enzymes that catalyze the hydrolysis of 3,'5'-cyclic nucleotides, such as cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), to their correspond...
Cell-free assay of G-protein-coupled receptors using fluorescence polarization [0.03%]
基于荧光偏振的无细胞G蛋白偶联受体活性检测法
Jessi Wildeson Jones,Tiffani A Greene,Christine A Grygon et al.
Jessi Wildeson Jones et al.
A recently developed nanotechnology, the Integral Molecular lipoparticle, provides an essentially soluble cell-free system in which G-protein-coupled receptors (GPCRs) in their native conformations are concentrated within virus-like particl...
Novel analytic criteria and effective plate designs for quality control in genome-scale RNAi screens [0.03%]
基因规模RNAi筛选中的质量控制的新分析标准和有效平板设计方法
Xiaohua Douglas Zhang
Xiaohua Douglas Zhang
One of the most fundamental challenges in genome-wide RNA interference (RNAi) screens is to glean biological significance from mounds of data, which relies on the development and adoption of appropriate analytic methods and designs for qual...
Application of a high-content multiparameter cytotoxicity assay to prioritize compounds based on toxicity potential in humans [0.03%]
通过高内涵多参数细胞毒性分析法基于人类潜在毒性进行化合物优先级划分的应用
Vivek C Abraham,Danli L Towne,Jeffrey F Waring et al.
Vivek C Abraham et al.
Prioritization of compounds based on human hepatotoxicity potential is currently a key unmet need in drug discovery, as it can become a major problem for several lead compounds in later stages of the drug discovery pipeline. The authors rep...
High-content fluorescent-based assay for screening activators of DNA damage checkpoint pathways [0.03%]
基于荧光的高内涵筛选DNA损伤检查点通路活化剂的方法
Bin Zhang,Xiubin Gu,Uma Uppalapati et al.
Bin Zhang et al.
Activation of DNA damage checkpoint pathways, including Chk2, serves as an anticancer barrier in precancerous lesions. In an effort to identify small-molecule activators of Chk2, the authors developed a quantitative cell-based assay using a...
Characterization of the 5-HT2b receptor in evaluation of aequorin detection of calcium mobilization for miniaturized GPCR high-throughput screening [0.03%]
G蛋白偶联受体高通量筛选中aequorin检测钙动员对5-HT2B受体的表征研究
Mark A Gilchrist nd,Angela Cacace,David G Harden
Mark A Gilchrist nd
Fluorescent detection of calcium mobilization has been used successfully to identify modulators of G-protein-coupled receptors (GPCRs); however, inherent issues with fluorescence may limit its potential for high-throughput screening miniatu...
2-tier bacterial and in vitro selection of active and methotrexate-resistant variants of human dihydrofolate reductase [0.03%]
两轮细菌和体外筛选高活性及甲氨蝶呤抗性的二氢叶酸还原酶变异文库
Elena Fossati,Jordan P Volpato,Lucie Poulin et al.
Elena Fossati et al.
We report a rapid and reliable 2-tier selection and screen for detection of activity as well as drug-resistance in mutated variants of a clinically-relevant drug-target enzyme. Human dihydrofolate reductase point-mutant libraries were subje...
Monoclonal antibody-based screening assay for factor inhibiting hypoxia-inducible factor inhibitors [0.03%]
基于单克隆抗体的低氧诱导因子抑制剂筛选试验
Sang-Hyeup Lee,Jeong Hee Moon,Eun Ah Cho et al.
Sang-Hyeup Lee et al.
The factor-inhibiting hypoxia-inducible factor (FIH) hydroxylates the asparagine 803 (Asn803) residue of the hypoxia-inducible factor 1alpha (HIF-1alpha), and the modification abrogates the transcriptional activity of HIF-1alpha. Because FI...