Screening for positive allosteric modulators: assessment of modulator concentration-response curves as a screening paradigm [0.03%]
正向别构调节剂的筛选：评估调节剂浓度-效应曲线作为筛选范式的应用
Christopher J Langmead
Christopher J Langmead
Targeting allosteric binding sites represents a powerful mechanism for selectively modulating receptor function. The advent of functional assays as the screening method of choice is leading to an increase in the number of allosteric modulat...
High-throughput screening for norepinephrine transporter inhibitors using the FLIPRTetra [0.03%]
采用FLIPRTetra高通量筛选去甲肾上腺素转运蛋白抑制剂
Ryan Wagstaff,Michael Hedrick,Jun Fan et al.
Ryan Wagstaff et al.
Monoamine transporters regulate the concentration of neurotransmitters in the synapse following neurotransmission and are very important drug targets in the pharmaceutical industry. Because of the labor-intensive nature of functional uptake...
Enhancing recombinant protein quality and yield by protein stability profiling [0.03%]
利用蛋白质稳定性谱图提高重组蛋白的产量和质量
Tara M Mezzasalma,James K Kranz,Winnie Chan et al.
Tara M Mezzasalma et al.
The reliable production of large amounts of stable, high-quality proteins is a major challenge facing pharmaceutical protein biochemists, necessary for fulfilling demands from structural biology, for high-throughput screening, and for assay...
A simple, no-wash cell adhesion-based high-throughput assay for the discovery of small-molecule regulators of the integrin CD11b/CD18 [0.03%]
一种简单的基于整合素CD11b/CD18的无洗细胞粘附高通量筛选小分子调节剂的方法
Jun Y Park,M Amin Arnaout,Vineet Gupta
Jun Y Park
The leukocyte-specific integrin CD11b/CD18 plays a key role in the biological function of these cells and represents a validated therapeutic target for inflammatory diseases. Currently, the low affinity interaction between CD11b/CD18 integr...
Expression of human nuclear receptors in plants for the discovery of plant-derived ligands [0.03%]
在植物中表达人核受体以发现来源于植物的配体
Elena V Doukhanina,Nestor R Apuya,Hye-Dong Yoo et al.
Elena V Doukhanina et al.
Plants have the potential to produce a wide array of secondary metabolites that have utility as drugs to treat human diseases. To tap this potential, functional human nuclear receptors have been expressed in plants to create in planta scree...
"Plate cherry picking": a novel semi-sequential screening paradigm for cheaper, faster, information-rich compound selection [0.03%]
“盘式捡樱桃法”：一种新型半顺序筛选模式实现低成本、快速且信息量丰富的化合物选择
Thomas J Crisman,Jeremy L Jenkins,Christian N Parker et al.
Thomas J Crisman et al.
This work describes a novel semi-sequential technique for in silico enhancement of high-throughput screening (HTS) experiments now employed at Novartis. It is used in situations in which the size of the screen is limited by the readout (e.g...
Discovery of ligands for Nurr1 by combined use of NMR screening with different isotopic and spin-labeling strategies [0.03%]
结合不同同位素和自旋标记的NMR筛选法发现Nurr1配体
Leszek Poppe,Timothy S Harvey,Christopher Mohr et al.
Leszek Poppe et al.
A comprehensive approach to target screening, hit validation, and binding site determination by nuclear magnetic resonance (NMR) spectroscopy is presented. NMR (19)F signal perturbation was used to screen a small compound library and identi...
Kristina Uvebrant,Dorthe da Graça Thrige,Anna Rosén et al.
Kristina Uvebrant et al.
Protein-protein interactions are widely found in biological systems controlling diverse cellular events. Because these interactions are implicated in many diseases such as autoimmunity and cancer, regulation of protein-protein interactions ...
The use of strictly standardized mean difference for hit selection in primary RNA interference high-throughput screening experiments [0.03%]
严格标准化均值差异在初级RNA干扰高通量筛选实验中的命中选择应用
Xiaohua Douglas Zhang,Marc Ferrer,Amy S Espeseth et al.
Xiaohua Douglas Zhang et al.
RNA interference (RNAi) high-throughput screening (HTS) has been hailed as the 2nd genomics wave following the 1st genomics wave of gene expression microarrays and single-nucleotide polymorphism discovery platforms. Following an RNAi HTS, t...
A support vector machine classifier for recognizing mitotic subphases using high-content screening data [0.03%]
基于高通量筛选数据识别有丝分裂亚期的支持向量机分类器
Charles Y Tao,Jonathan Hoyt,Yan Feng
Charles Y Tao
High-content screening studies of mitotic checkpoints are important for identifying cancer targets and developing novel cancer-specific therapies. A crucial step in such a study is to determine the stage of cell cycle. Due to the overwhelmi...