Binding of a Pleckstrin homology domain protein to phosphoinositide in membranes: a miniaturized FRET-based assay for drug screening [0.03%]
基于FRET的药物筛选微型化膜结合试验及其在磷脂酰肌醇结合蛋白中的应用
Brian D Hamman,Brian A Pollok,Todd Bennett et al.
Brian D Hamman et al.
Pleckstrin homology (PH) domains are present in key proteins involved in many vital cell processes. For example, the PH domain of Bruton's tyrosine kinase (Btk) binds to phosphatidylinositol triphosphate (PIP(3)) in the plasma membrane afte...
A homogeneous high throughput nonradioactive method for measurement of functional activity of Gs-coupled receptors in membranes [0.03%]
一种均相的高通量非放射性方法 用于测量膜中Gs偶联受体的功能活性
Michael Allen,David Hall,Barbara Collins et al.
Michael Allen et al.
A method is described for measuring the activity of G(s)-coupled receptors in a nonradioactive homogeneous membrane-based assay. This method has several major advantages over currently used methods for measuring functional activity of G(s)-...
Microplate screening of the differential effects of test agents on Hoechst 33342, rhodamine 123, and rhodamine 6G accumulation in breast cancer cells that overexpress P-glycoprotein [0.03%]
荧光微孔板筛选试验药物在乳腺癌细胞中对Hoechst 33342、Rhodamine 123和Rhodamine 6G蓄积的差异性影响
Jeffrey G Sarver,Wieslaw A Klis,James P Byers et al.
Jeffrey G Sarver et al.
A microplate screening method has been developed to evaluate the effects of test agents on the accumulation of the fluorescent P-glycoprotein (Pgp) substrates Hoechst 33342, rhodamine 123, and rhodamine 6G in multidrug-resistant (MDR) breas...
Determination of ligand-MurB interactions by isothermal denaturation: application as a secondary assay to complement high throughput screening [0.03%]
用等温变性法测定配体与MurB的结合：作为高通量筛选的补充次级试验的方法学应用研究
Ronald W Sarver,Joseph M Rogers,Dennis E Epps
Ronald W Sarver
We used a temperature-jump isothermal denaturation procedure with various methods of detection to evaluate the quality of putative inhibitors of MurB discovered by high-throughput screening. Three optical methods of detection-ultraviolet hy...
Automated high throughput screening for serine kinase inhibitors using a LEADseeker scintillation proximity assay in the 1536-well format [0.03%]
采用LEADseeker闪烁邻近技术在1536孔板中筛选丝氨酸激酶抑制剂的高通量方法
Gabriele Sorg,Hans-Dieter Schubert,Frank H Büttner et al.
Gabriele Sorg et al.
High-throughput screening in the 1536-well format has been largely restricted to solution-based and cell-based screens. In this article, we show the feasibility of a completely automated, robust scintillation proximity assay in the 1536-wel...
A comparison of ALPHAScreen, TR-FRET, and TRF as assay methods for FXR nuclear receptors [0.03%]
AlphaScreen、TR-FRET和TRF作为FXR核受体测定方法的比较研究
J Fraser Glickman,Xiang Wu,Robert Mercuri et al.
J Fraser Glickman et al.
New developments in detection technologies are providing a variety of biomolecular screening strategies from which to choose. Consequently, we performed a detailed analysis of both separation-based and non-separation-based formats for scree...
Comparative Study
Journal of biomolecular screening. 2002 Feb;7(1):3-10. DOI:10.1177/108705710200700102 2002
High-density miniaturized thermal shift assays as a general strategy for drug discovery [0.03%]
高密度小型化热移位测定法作为一种通用的药物发现策略
M W Pantoliano,E C Petrella,J D Kwasnoski et al.
M W Pantoliano et al.
More general and universally applicable drug discovery assay technologies are needed in order to keep pace with the recent advances in combinatorial chemistry and genomics-based target generation. Ligand-induced conformational stabilization...
High throughput studies of gene expression using green fluorescent protein-oxidative stress promoter probe constructs: the potential for living chips [0.03%]
用于绿色荧光蛋白-氧化应激启动子探针结构的基因表达高通量研究及活芯片的可能性
C R Albano,C Lu,W E Bentley et al.
C R Albano et al.
Green fluorescent protein fusions were constructed with several oxidative stress promoters from Escherichia coli. These promoters were chosen for their induction by reactive oxygen species (ROS) such as superoxide, hydrogen peroxide, and hy...
High throughput fluorescence assays for the measurement of mitochondrial activity in intact human neuroblastoma cells [0.03%]
高通量荧光测定法检测完整的人类神经母细胞瘤线粒体活性
A J Woollacott,P B Simpson
A J Woollacott
The mitochondrial permeability transition event is implicated in the activation phase of apoptosis and necrosis, and is therefore postulated to play a role in many disease states. Mitochondrial permeability transition is therefore of increa...
Application of beta-galactosidase enzyme complementation technology as a high throughput screening format for antagonists of the epidermal growth factor receptor [0.03%]
β-半乳糖苷酶酶互补技术在表皮生长因子受体拮抗剂高通量筛选中的应用
D L Graham,N Bevan,P N Lowe et al.
D L Graham et al.
We have applied enzyme complementation technology to develop a screen for antagonists of the epidermal growth factor (EGF) receptor. Chimeric proteins containing two weakly complementing deletion mutants of Escherichia coli beta-galactosida...