Kaja K Selmer,Kristin Brandal,Ole K Olstad et al.
Kaja K Selmer et al.
Single nucleotide polymorphisms (SNPs) have recently replaced microsatellites as the genetic markers of choice in linkage analysis, primarily because they are more abundant and the genotypes more amenable for automatic calling. One of the m...
Optimizing the expression of recombinant alphabetagamma GABAA receptors in HEK293 cells for high-throughput screening [0.03%]
在HEK293细胞中优化重组alphabetagamma GABAA受体的表达，用于高通量筛选
Daniel Gilbert,Abolghasem Esmaeili,Joseph W Lynch
Daniel Gilbert
Despite being important clinical targets, it is not straightforward to reliably express recombinant trimeric alphabetagamma GABA-A receptors (GABA(A)Rs) for high-throughput screening. This study therefore sought to devise a simple and relia...
Elizabeth B Gottlin,Xiangrong Guan,Charles Pegram et al.
Elizabeth B Gottlin et al.
Epidermal growth factor receptor (EGFR) is overexpressed or mutated in a high percentage of tumors. EGFR has long been considered a promising target for cancer diagnostic and therapeutic applications. However, monoclonal antibodies and othe...
Process validation and screen reproducibility in high-throughput screening [0.03%]
高通量筛选中的工艺验证与屏幕重复性
Isabel Coma,Liz Clark,Emilio Diez et al.
Isabel Coma et al.
The use of large-scale compound screening has become a key component of drug discovery projects in both the pharmaceutical and the biotechnological industries. More recently, these activities have also been embraced by the academic communit...
Comparison of variability and sensitivity between nuclear translocation and luciferase reporter gene assays [0.03%]
核转位与荧光素酶报告基因检测的差异性和敏感性比较研究
Vincent Unterreiner,Yvonne Ibig-Rehm,Marjo Simonen et al.
Vincent Unterreiner et al.
High-content screening (HCS), a technology based on subcellular imaging by automated microscopy and sophisticated image analysis, has emerged as an important platform in small-molecule screening for early drug discovery. To validate a subce...
Comparative Study
Journal of biomolecular screening. 2009 Jan;14(1):59-65. DOI:10.1177/1087057108328016 2009
Characterizing cannabinoid CB2 receptor ligands using DiscoveRx PathHunter beta-arrestin assay [0.03%]
使用DiscoveRx PathHunter β- arrestin测定法表征大麻素CB2受体配体
Debra McGuinness,Asra Malikzay,Richard Visconti et al.
Debra McGuinness et al.
The authors have characterized a set of cannabinoid CB(2) receptor ligands, including triaryl bis sulfone inverse agonists, in a cell-based receptor/beta-arrestin interaction assay (DiscoveRx PathHunter). The results were compared with resu...
A high-throughput ligand competition binding assay for the androgen receptor and other nuclear receptors [0.03%]
一种针对雄激素受体及其他核受体的竞争性配体结合高通量筛选方法
Clémentine Féau,Leggy A Arnold,Aaron Kosinski et al.
Clémentine Féau et al.
Standardized, automated ligand-binding assays facilitate evaluation of endocrine activities of environmental chemicals and identification of antagonists of nuclear receptor ligands. Many current assays rely on fluorescently labeled ligands ...
Development and validation of a higher throughput screening approach to genotoxicity testing using the GADD45a-GFP GreenScreen HC assay [0.03%]
基于GADD45a-GFP GreenScreen HC测定的基因毒性筛查方法的开发和验证
Andrew W Knight,Louise Birrell,Richard M Walmsley
Andrew W Knight
There is a pressing need to develop rapid yet accurate screening assays for the identification of genotoxic liability and for early hazard assessment in drug discovery. The GADD45a-GFP human cell-based genotoxicity assay (GreenScreen HC) ha...
A fluorescence lifetime-based assay for protease inhibitor profiling on human kallikrein 7 [0.03%]
基于荧光寿命的人类蛋白酶抑制剂克林霉素7的测定法
Klaus Doering,Gabriele Meder,Manuela Hinnenberger et al.
Klaus Doering et al.
Fluorescence lifetime is an intrinsic parameter describing the fluorescence process. Changes in the fluorophore's physicochemical environment can lead to changes in the fluorescence lifetime. When used as the readout in biological assays, i...
High-throughput biochemical kinase selectivity assays: panel development and screening applications [0.03%]
高通量生化激酶选择性筛选体系的建立及应用
Amy Card,Chris Caldwell,Hyunsuk Min et al.
Amy Card et al.
Kinases represent attractive targets for drug discovery. Eight small-molecule kinase inhibitors are currently marketed in the area of oncology, and numerous others are in clinical trials. Characterization of the selectivity profiles of thes...