Robust hit identification by quality assurance and multivariate data analysis of a high-content, cell-based assay [0.03%]
高质量保证及多元统计分析在基于细胞的高通量筛选中的 hit 确认作用研究
Oliver Dürr,François Duval,Anthony Nichols et al.
Oliver Dürr et al.
Recent technological advances in high-content screening instrumentation have increased its ease of use and throughput, expanding the application of high-content screening to the early stages of drug discovery. However, high-content screens ...
Development and validation of a cell-based high-throughput screening assay for TRPM2 channel modulators [0.03%]
TRPM2通道调节剂的细胞基于高通量筛选测定的建立及验证
Yumei Song,Ben Buelow,Anne-Laure Perraud et al.
Yumei Song et al.
TRPM2 is a member of the transient receptor potential melastatin (TRPM)-related ion channel family. The activation of TRPM2 induced by oxidative/nitrosative stress leads to an increase in intracellular free Ca(2+). Although further progress...
Phage display screening of epithelial cell monolayers treated with EGTA: identification of peptide FDFWITP that modulates tight junction activity [0.03%]
EGTA处理的上皮细胞单层的噬菌体显示筛选：鉴定调节紧密连接活性的肽FDFWITP
Richard E Herman,Ekaterina G Makienko,Mary G Prieve et al.
Richard E Herman et al.
Phage display was used to screen for peptides that modulate the activity of epithelial cell tight junctions. Panning with a phage library that displays random 7-mers was performed using monolayers of human bronchial epithelial cells (16HBE1...
Screening for compounds that induce apoptosis of cancer cells grown as multicellular spheroids [0.03%]
筛选可诱导癌细胞球体凋亡的化合物
Richard Herrmann,Walid Fayad,Stephan Schwarz et al.
Richard Herrmann et al.
Screening and initial characterization of anticancer drugs are typically performed using monolayer cultures of tumor cells. It is well established that such monolayer cultures do not represent the characteristics of 3-dimensional solid tumo...
A high-content glucocorticoid receptor translocation assay for compound mechanism-of-action evaluation [0.03%]
一种用于化合物作用机制评价的高内涵糖皮质激素受体转位检测方法
Michele Agler,Margaret Prack,Yingjie Zhu et al.
Michele Agler et al.
Ligand-induced cytoplasm to nucleus translocation is a critical event in the nuclear receptor (NR) signal transduction cascade. The development of green fluorescent proteins and their color variants fused with NRs, along with the recent dev...
A high-throughput screen measuring ubiquitination of p53 by human mdm2 [0.03%]
一种用于测量由人MDM2诱导的p53泛素化的方法及其应用
Monique F Murray,Anthony J Jurewicz,John D Martin et al.
Monique F Murray et al.
Tumor suppressor p53 is typically maintained at low levels in normal cells. In response to cellular stresses, such as DNA damage, p53 is stabilized and can stimulate responses leading to cell cycle arrest or apoptosis. Corresponding to its ...
Development of in vitro pharmacokinetic screens using Caco-2, human hepatocyte, and Caco-2/human hepatocyte hybrid systems for the prediction of oral bioavailability in humans [0.03%]
一种体外药动学筛选方法的发展历程，采用Caco-2、人体肝细胞和Caco-2/人体肝细胞混合系统预测人类口服生物利用度
Cheng Li,Tongtong Liu,Xiaoming Cui et al.
Cheng Li et al.
In this study, in vitro systems were used to build 2 pharmacokinetic models that predict human oral bioavailability: the Caco-2/hepatocyte combination model and the Caco-2/hepatocyte hybrid model. Data obtained in vitro on Caco-2 cell perme...
Felipe De Almeida Dias,André Luis Souza Dos Santos,Antônio Ferreira-Pereira et al.
Felipe De Almeida Dias et al.
Adhesive interactions between cells are critical to a variety of processes, including host-pathogen relationships. The authors have developed a new technique for the observation of binding interactions in which molecules obtained from excis...
Mike Dragunow,Rachel Cameron,Pritika Narayan et al.
Mike Dragunow et al.
A number of biochemical methods are available for measuring fat accumulation in cell culture. The authors report a simple image-based method for measuring fat accumulation in adipocytes using a combination of high-throughput brightfield mic...
Detection of functional ligand-binding events using synchrotron x-ray scattering [0.03%]
采用同步辐射X射线散射技术检测功能配体结合事件
Diane J Rodi,Suneeta Mandava,David B Gore et al.
Diane J Rodi et al.
Small-molecule ligands that change the structure of a protein are likely to affect its function, whereas those causing no structural change are less likely to be functional. Wide-angle x-ray scattering (WAXS) can be easily carried out on pr...