High-throughput identification of inhibitors of human mitochondrial peptide deformylase [0.03%]
人类线粒体肽脱甲酰基酶抑制剂的高效筛选体系及虚拟筛选
Christophe Antczak,David Shum,Sindy Escobar et al.
Christophe Antczak et al.
The human mitochondrial peptide deformylase (HsPDF) provides a potential new target for broadly acting antiproliferative agents. To identify novel nonpeptidomimetic and nonhydroxamic acid-based inhibitors of HsPDF, the authors have develope...
Optimization procedure for small interfering RNA transfection in a 384-well format [0.03%]
一种在384孔板中进行小干扰RNA转染的优化方法
Jason Borawski,Alicia Lindeman,Frank Buxton et al.
Jason Borawski et al.
High-throughput screening of RNAi libraries has become an essential part of functional analysis in academic and industrial settings. The transition of a cell-based RNAi assay into a 384-well format requires several optimization steps to ens...
Development of a Transcreener kinase assay for protein kinase A and demonstration of concordance of data with a filter-binding assay format [0.03%]
TRANCEAVER酶联免疫吸附检测法(PKA)的研发及与滤膜结合测定法数据一致性的验证
Karen L Huss,Pauline E Blonigen,Robert M Campbell
Karen L Huss
A Transcreener kinase fluorescence polarization (FP) assay has been developed for the serine/threonine kinase protein kinase A (PKA). The PKA Transcreener kinase assay is an homogenous, competitive antibody-based FP assay that uses Far Red ...
Comparative Study
Journal of biomolecular screening. 2007 Jun;12(4):578-84. DOI:10.1177/1087057107300221 2007
Development of a homogeneous time-resolved fluorescence leukotriene B4 assay for determining the activity of leukotriene A4 hydrolase [0.03%]
均一型时间分辨荧光 leukotriene B4 测定法在确定 leukotriene A4 水解酶活性中的应用开发研究
Amy M Liang,Emmanuel Claret,Josy Ouled-Diaf et al.
Amy M Liang et al.
Leukotriene A4 (LTA4) hydrolase catalyzes a rate-limiting final biosynthetic step of leukotriene B4 (LTB4), a potent lipid chemotactic agent and proinflammatory mediator. LTB4 has been implicated in the pathogenesis of various acute and chr...
Comparative Study
Journal of biomolecular screening. 2007 Jun;12(4):536-45. DOI:10.1177/1087057107299873 2007
Gene expression profiling of rheumatoid arthritis synovial cells treated with antirheumatic drugs [0.03%]
抗风湿药物处理类风湿关节炎滑膜细胞的基因表达谱分析
Thomas Häupl,Mehdi Yahyawi,Carsten Lübke et al.
Thomas Häupl et al.
Nonbiological therapeutics are frequently used for the treatment of patients with rheumatoid arthritis (RA). Because the mechanisms of action of these therapeutics are unclear, the authors aimed to elucidate the molecular effects of typical...
Discovery of a novel small-molecule targeting selective clearance of mutant huntingtin fragments [0.03%]
靶向选择清除突变亨廷顿蛋白片段的小分子物质的新发现
Myra Coufal,Michele M Maxwell,Deborah E Russel et al.
Myra Coufal et al.
CAG-triplet repeat extension, translated into polyglutamines within the coding frame of otherwise unrelated gene products, causes 9 incurable neurodegenerative disorders, including Huntington's disease. Although an expansion in the CAG repe...
Online biochemical detection of glutathione-S-transferase P1-specific inhibitors in complex mixtures [0.03%]
复杂混合物中谷胱甘肽S转移酶P1特异性抑制剂的在线生化检测法
Jeroen Kool,Mark Eggink,Huub van Rossum et al.
Jeroen Kool et al.
A high-resolution screening (HRS) technology is described, which couples 2 parallel enzyme affinity detection (EAD) systems for substrates and inhibitors of rat cytosolic glutathione-S-transferases (cGSTs) and purified human GST P1 to gradi...
Pharmacological characterization of a fluorescent uptake assay for the noradrenaline transporter [0.03%]
noradrenaline transporter的荧光摄取试验的药理表征
Anders Haunsø,Dawn Buchanan
Anders Haunsø
The noradrenaline transporter (NET) is a Na(+)/Cl(-) dependent monoamine transporter that mediates rapid clearance of noradrenaline from the synaptic cleft, thereby terminating neuronal signaling. NET is an important target for drug develop...
A nuclear magnetic resonance-based functional assay for nicotinamide adenine dinucleotide synthetase [0.03%]
基于核磁共振的烟酸腺嘌呤二核苷酸合酶功能测定法
Brian J Stockman,Ian J Lodovice,Douglas A Fisher et al.
Brian J Stockman et al.
Nicotinamide adenine dinucleotide synthetase (NadE) is an essential enzyme for bacterial pathogens and is thus a promising antibacterial target. It catalyzes the conversion of nicotinic acid adenine dinucleotide to nicotinamide adenine dinu...
High-throughput determination of mode of inhibition in lead identification and optimization [0.03%]
hit发现与优化中高通量测定抑制类型的方法
Min Wei,Richard Wynn,Gregory Hollis et al.
Min Wei et al.
After finishing the primary high-throughput screening, the screening team is often faced with thousands of hits to be evaluated further. Effective filtering of these hits is crucial in identifying leads. Mode of inhibition (MOI) study is ex...
Comparative Study
Journal of biomolecular screening. 2007 Mar;12(2):220-8. DOI:10.1177/1087057106296679 2007