Development of a plasmepsin II fluorescence polarization assay suitable for high throughput antimalarial drug discovery [0.03%]
一种适用于高效抗疟疾药物发现的针对Plasmepsin II的荧光偏振检测方法的研究与发展
Horst Flotow,Chung-Yan Leong,Antony D Buss
Horst Flotow
Despite decades of research, malaria remains the world's most deadly parasitic disease. New treatments with novel mechanisms of action are urgently needed. Plasmepsin II is an aspartyl protease that has been validated as an antimalarial the...
Jonathan M Evans,Phillip G Zaworski,Christian N Parker
Jonathan M Evans
Fungal cell wall synthesis is essential for viability, requiring the activity of genes involved in environmental sensing, precursor synthesis, transport, secretion, and assembly. This multitude of potential targets, the availability of know...
Detlef Thoenges,Andreas Barth
Detlef Thoenges
A direct approach to enzyme activity measurements is presented. Vibrational spectroscopy can monitor the progress of enzymatic reactions because the vibrational spectrum of substrates and products usually differs. This is demonstrated by th...
Michael F M Engels,Luc Wouters,Rudi Verbeeck et al.
Michael F M Engels et al.
A data mining procedure for the rapid scoring of high-throughput screening (HTS) compounds is presented. The method is particularly useful for monitoring the quality of HTS data and tracking outliers in automated pharmaceutical or agrochemi...
Selective cytotoxicity evaluation in anticancer drug screening of fractionated plant extracts [0.03%]
基于分数植物提取物的抗癌药物筛选中的选择性细胞毒性评价
Petra Lindholm,Joachim Gullbo,Per Claeson et al.
Petra Lindholm et al.
Chosen to reflect biodiversity in a phylogenetic sense, 100 fractionated plant extracts were screened in vitro for cytotoxicity following extraction and fractionation (polypeptide isolation). Of these 100 extracts, 30 were selected and then...
Development of a keratinocyte-based screening model for antipsoriatic drugs using green fluorescent protein under the control of an endogenous promoter [0.03%]
开发一种基于角质细胞的抗银屑病药物筛选模型采用绿色荧光蛋白受内源性启动子控制
Arno Pol,Fred van Ruissen,Joost Schalkwijk
Arno Pol
Inflamed epidermis (psoriasis, wound healing, ultraviolet-irradiated skin) harbors keratinocytes that are hyperproliferative and display an abnormal differentiation program. A distinct feature of this so-called regenerative maturation pathw...
Application of Micro Arrayed Compound Screening (microARCS) to identify inhibitors of caspase-3 [0.03%]
应用微阵列化合物筛选(microARCS)技术鉴定caspase-3抑制剂
Sujatha M Gopalakrishnan,Jarkko Karvinen,James L Kofron et al.
Sujatha M Gopalakrishnan et al.
Micro Arrayed Compound Screening (microARCS) is a miniaturized ultra-high-throughput screening platform developed at Abbott Laboratories. In this format, 8,640 discrete compounds are spotted and dried onto a polystyrene sheet, which has the...
Sandra Fox,Helen Wang,Lynne Sopchak et al.
Sandra Fox et al.
Serotonin antagonist profiling on 5HT2A and 5HT2C receptors by nonequilibrium intracellular calcium response using an automated flow-through fluorescence analysis system, HT-PS 100 [0.03%]
利用自动化流动注射荧光分析系统对血清素拮抗剂在5-HT2A和5-HT2C受体上的非平衡胞内钙反应进行受体筛选研究-HT-PS 100
Gregory Kaler,Michael Otto,Alex Okun et al.
Gregory Kaler et al.
Characterization of the potencies of agonists and antagonists in cell-based assays can be complicated by nonequilibrium conditions of functional response. We assessed the potencies of a series of serotonin (5HT) antagonists by inhibition of...
Pharmacological comparison of a recombinant CB1 cannabinoid receptor with its G(alpha 16) fusion product [0.03%]
CB1型大麻素受体及其与G(alpha 16)融合产物的药理学比较研究
Renée S Martin,Paul H Reynen,Joyce J Calixto et al.
Renée S Martin et al.
The pharmacology of G protein-coupled receptors is widely accepted to depend on the G protein subunit to which the agonist-stimulated receptor couples. In order to investigate whether CB(1) agonist-mediated signal transduction via an engine...
Comparative Study
Journal of biomolecular screening. 2002 Jun;7(3):281-9. DOI:10.1177/108705710200700312 2002