Mouse thymus targeted peptide isolated by in vivo phage display can inhibit bioactivity of thymus output in vivo [0.03%]
一种体内噬菌体展示筛选的胸腺靶向多肽能够抑制胸腺输出功能
Yang Yu,Zizheng Wang,Tongxin Du
Yang Yu
Heterogeneity of the vasculature in different organs has been well documented by the method of in vivo phage display. Using this technology, several peptide ligands that home to tissue-specific vascular endothelial cell have been isolated. ...
Identification of small molecule inhibitors of the mitotic kinase haspin by high-throughput screening using a homogeneous time-resolved fluorescence resonance energy transfer assay [0.03%]
基于同源时间分辨荧光共振能量转移检测的高通量筛选小分子化合物抑制细胞有丝分裂激酶haspin的方法及用途
Debasis Patnaik,Jun Xian,Marcie A Glicksman et al.
Debasis Patnaik et al.
Haspin/Gsg2 is a kinase that phosphorylates histone H3 at Thr-3 (H3T3ph) during mitosis. Its depletion by RNA interference results in failure of chromosome alignment and a block in mitosis. Haspin, therefore, is a novel target for developme...
Template-directed self-assembly enhances RTK catalytic domain function [0.03%]
模板导向的自组装增强受体酪氨酸激酶催化结构域功能
Edward A Esposito,Anthony L Shrout,Robert M Weis
Edward A Esposito
Receptor tyrosine kinases have become important therapeutic targets because of their involvement in diseases, including cancer. Kinase domains, which are soluble and easily purified, have found widespread use in enzyme inhibitor assays, but...
Catalytically active peptidylglycine alpha-amidating monooxygenase in the media of androgen-independent prostate cancer cell lines [0.03%]
雄激素非依赖性前列腺癌细胞系培养上清中具有催化活性的肽基精氨酶多功能氧化酶(PAM)
Jill A Trendel,Nicole Ellis,Jeffrey G Sarver et al.
Jill A Trendel et al.
Peptidylglycine alpha-amidating monooxygenase (PAM) converts inactive terminal-glycine prohormones into their activated alpha-amidated forms. PAM is thought to play a role in the development of antiandrogen drug resistance in prostate cance...
A novel high-throughput screening assay for putative antidiabetic agents through PPARalpha interactions [0.03%]
一种通过PPARα相互作用筛选假定抗糖尿病制剂的新型高效筛选试验
Heather A Hostetler,Lindsay R Syler,Lindy N Hall et al.
Heather A Hostetler et al.
As natural peroxisome proliferator-activated receptor-alpha (PPARalpha) ligands, high levels of fatty acids and glucose could lead to hyperactivation of PPARalpha, like that seen in diabetes. Important diabetes research goals are to uncover...
Activation and translocation of glucokinase in rat primary hepatocytes monitored by high content image analysis [0.03%]
高内容图像分析在大鼠肝细胞原代培养中激活并转位的己糖激酶的研究
Michael Wolff,Stefan G Kauschke,Susanne Schmidt et al.
Michael Wolff et al.
In the liver, glucokinase (GK) regulatory protein (GKRP) negatively modulates the metabolic enzyme GK by locking it in an inactive state in the nucleus. Here, the authors established a high content screening assay in the 384-well microplate...
Demonstration of improvements to the bioluminescence resonance energy transfer (BRET) technology for the monitoring of G protein-coupled receptors in live cells [0.03%]
G蛋白偶联受体活细胞检测的生物发光共振能量转移(BRET)技术改进演示
Martina Kocan,Heng B See,Ruth M Seeber et al.
Martina Kocan et al.
The bioluminescence resonance energy transfer (BRET) technique has become extremely popular for studying protein-protein interactions in living cells and real time. Of particular interest is the ability to monitor interactions between G pro...
High-throughput microsomal stability assay for screening new chemical entities in drug discovery [0.03%]
一种用于药物发现中高通量筛选新化学实体的微粒体稳定性试验方法
Massimiliano Fonsi,Maria V Orsale,Edith Monteagudo
Massimiliano Fonsi
In this work, the authors present a novel, robotic, automated protocol for assessing a metabolic stability protocol assembled on a Hamilton platform and a new strategy for pooling samples (cassette analysis). To increase the high throughput...
The application of an immobilized molecular beacon for the analysis of the DNA binding domains from the ecdysteroid receptor proteins Usp and EcR's interaction with the hsp27 response element [0.03%]
分子信标在保幼激素受体蛋白Usp和EcR结合于hsp27反应原件的DNA结区域分析中的应用研究
Tomasz Krusiński,Anna Laskowska,Andrzej Ozyhar et al.
Tomasz Krusiński et al.
The nonstandard molecular beacon described in this article consists of 2 fragments, each built of a short single-stranded oligonucleotide sequence and a double-stranded sequence. One of these hybridization probes, labeled with a fluorescenc...
High-throughput screening of a 100,000-compound library for inhibitors of influenza A virus (H3N2) [0.03%]
用于筛选抑制流感病毒(A型(H3N2))的化合物库的高通量方法(10万种化合物)
William E Severson,Michael McDowell,Subramaniam Ananthan et al.
William E Severson et al.
Using a highly reproducible and robust cell-based high-throughput screening (HTS) assay, the authors screened a 100,000-compound library at 14- and 114-microM compound concentration against influenza strain A/Udorn/72 (H3N2). The "hit" rate...