High throughput screening method for identification of new lipofection reagents [0.03%]
新的脂质转染试剂识别的高通量筛选方法
A E Regelin,E Fernholz,H F Krug et al.
A E Regelin et al.
Lipofection, the transfer of genetic material into cells by means of cationic lipids, is of growing interest for in vitro and in vivo approaches. In order to identify ideal lipofection reagents in a HTS, we have developed an automated lipof...
Identification of inhibitors of bacterial transcription/translation machinery utilizing a miniaturized 1536-well format screen [0.03%]
利用小型化的1536孔板筛选鉴定细菌转录/翻译机器的抑制剂
I Kariv,H Cao,P D Marvil et al.
I Kariv et al.
This report presents the miniaturization of a HTS screen to identify inhibitors of prokaryotic transcription-translation in a 1536-well format. The in vitro assay design utilized the bacterial expression machinery to drive expression of a f...
The potential for CYP2D6 inhibition screening using a novel scintillation proximity assay-based approach [0.03%]
一种新的CYP2D6抑制筛查方法——基于闪烁邻近技术的应用潜力分析
E Delaporte,D E Slaughter,M A Egan et al.
E Delaporte et al.
High throughput inhibition screens for human cytochrome P450s (CYPs) are being used in preclinical drug metabolism to support drug discovery programs. The versatility of scintillation proximity assay (SPA) technology has enabled the develop...
A versatile high throughput screen for dioxygenase activity using solid-phase digital imaging [0.03%]
一种使用固相数字成像的高效筛选脱氢酶活性的方法
J M Joern,T Sakamoto,A Arisawa et al.
J M Joern et al.
We have developed a solid-phase, high throughput (10,000 clones/day) screen for dioxygenase activity. The cis-dihydrodiol product of dioxygenase bioconversion is converted to a phenol by acidification or to a catechol by reaction with cis-d...
G P Sabbatini,W A Shirley,D L Coffen
G P Sabbatini
Producing quality clinical candidates less prone to late stage failure is greatly facilitated by better integration of the relevant high throughput functions and the inclusion of ADME/toxicology further upstream in the discovery process. We...
High throughput prediction of oral absorption: improvement of the composition of the lipid solution used in parallel artificial membrane permeation assay [0.03%]
基于平行人工膜渗透法的口服吸收预测的高通量筛选及其脂质溶液组成的优化研究
K Sugano,H Hamada,M Machida et al.
K Sugano et al.
The purpose of the present study was to improve the composition of the lipid solution used in parallel artificial membrane permeation assay for the precise prediction of oral absorption. We modified the composition of lipid solution, which ...
Merged screening for human immunodeficiency virus Tat and Rev inhibitors [0.03%]
人免疫缺陷病毒Tat和Rev抑制剂的联合筛选方法
F Hamy,E Felder,K Lipson et al.
F Hamy et al.
In addition to "conventional" drug discovery targets used in modern strategies, mainly focusing on proteins, recent insights into gene regulation as a novel drug concept have begun to invite the targeting of biomolecular interactions betwee...
Development of a high throughput screening assay for inhibitors of fibroblast growth factor-receptor-heparin interactions [0.03%]
高效筛选抑制成纤维细胞生长因子受体肝素相互作用的抑制剂的方法的发展
D Aviezer,A P Seddon,M J Wildey et al.
D Aviezer et al.
High throughput screening (HTS) of large compound libraries for inhibitors of growth factors raises the requirement for simple yet reliable assays. Fibroblast growth factors (FGFs) play a pivotal role in the multistep pathway of malignant t...
Ligand binding to transmembrane receptors on intact cells or membrane vesicles measured in a homogeneous 1-microliter assay format [0.03%]
用于整体细胞或膜小泡的跨膜受体配体结合的均相1微升测定格式筛查分子库
M Klumpp,A Scheel,E Lopez-Calle et al.
M Klumpp et al.
We have developed homogeneous miniaturized assays to measure ligand binding to either intact cells or receptor-containing membrane fragments by analysis of particle brightness. As an example, the affinities and inhibition constants of fluor...
Development of a fluorescence based high throughput assay for antagonists of the human chorionic gonadotropin receptor extracellular domain: analysis of peptide inhibitors [0.03%]
一种基于荧光的人绒毛膜促性腺激素受体细胞外结构域拮抗剂高通量分析法的开发：肽抑制剂分析
L I Lobel,J P Morseman,X Zeng et al.
L I Lobel et al.
A simple method for prompt fluorescent detection of inhibitors of human chorionic gonadotropin (hCG) binding to the extracellular domain of the human luteinizing hormone/chorionic gonadotropin (hLH/CG) receptor was developed for high throug...