Homogeneous time-resolved fluorescence resonance energy transfer assay for measurement of Phox/Bem1p (PB1) domain heterodimerization [0.03%]
同种时间分辨荧光共振能量转移测定法测定Phox/Bem1p(PB1)结构域异二聚体形成
Kazuhiro Nakamura,Jon S Zawistowski,Mark A Hughes et al.
Kazuhiro Nakamura et al.
Twenty human proteins encode Phox/Bem1p (PB1) domains, which are involved in forming protein heterodimers. MEKK2, MEKK3, and MEK5 are 3 serine-threonine protein kinases that have PB1 domains. MEKK2, MEKK3, and MEK5 are the MAP3Ks and the MA...
Homogeneous time-resolved fluorescence resonance energy transfer assay for measurement of Phox/Bem1p (PB1) domain heterodimerization [0.03%]
用于测定Phox/Bem1p(PB1)结构域异二聚体形成的均相时间分辨荧光共振能量转移法
Kazuhiro Nakamura,Jon S Zawistowski,Mark A Hughes et al.
Kazuhiro Nakamura et al.
Twenty human proteins encode Phox/Bem1p (PB1) domains, which are involved in forming protein heterodimers. MEKK2, MEKK3, and MEK5 are 3 serine-threonine protein kinases that have PB1 domains. MEKK2, MEKK3, and MEK5 are the MAP3Ks and the MA...
Evaluation of fluorescence- and mass spectrometry-based CYP inhibition assays for use in drug discovery [0.03%]
用于药物发现的荧光和质谱基CYP抑制评估检测的方法学研究
Leslie Bell,Shari Bickford,Phong Hung Nguyen et al.
Leslie Bell et al.
The potential for metabolism-related drug-drug interactions by new chemical entities is assessed by monitoring the impact of these compounds on cytochrome P450 (CYP) activity using well-characterized CYP substrates. The conventional gold st...
Use of cryopreserved cells for enabling greater flexibility in compound profiling [0.03%]
利用cryopreserved细胞提高化合物筛选的灵活性
M J Wigglesworth,K J Lawless,D J Standing et al.
M J Wigglesworth et al.
Measurement of intracellular calcium release following agonist challenge within cells expressing the relevant membrane protein is a commonly used format to derive structure-activity relationship (SAR) data within a compound profiling assay....
Development of a homogeneous high-throughput live-cell G-protein-coupled receptor binding assay [0.03%]
均一高通量活细胞G蛋白偶联受体结合分析的建立和发展
Paul H Lee,Steven C Miller,Carlo van Staden et al.
Paul H Lee et al.
The measurement of ligand receptor binding parameters for G-protein-coupled receptors is indispensable in the drug discovery process. Traditional ligand receptor binding assays require scale-up of cells and membrane preparations, which is a...
Application of high-throughput isothermal denaturation to assess protein stability and screen for ligands [0.03%]
高温高通量恒温变性技术及其在蛋白质稳定性检测及配体筛选中的应用
Guillermo A Senisterra,Bum Soo Hong,Hee-Won Park et al.
Guillermo A Senisterra et al.
Many diseases in humans are caused by mutations that decrease the stability of specific proteins or increase their susceptibility to aggregation. Consequently, the availability of high-throughput methods for assessing protein stability and ...
Ho Yan Gloria Tse,Vincent Wai Tsun Li,Michelle N Y Hui et al.
Ho Yan Gloria Tse et al.
Chinese materia medica (CMM) is becoming increasingly important in modern health care, with the potential for new or improved clinical protocols and reduction in treatment costs. Conventional approaches to drug discovery are based on knowle...
A method with flexible and balanced control of false negatives and false positives for hit selection in RNA interference high-throughput screening assays: a statistical terminology [0.03%]
一种在RNA干扰高通量筛选实验中选择阳性孔的、可灵活调节假阳孔与假阴孔概率的方法及其统计学原理
Edna Schechtman
Edna Schechtman
Zhang suggests a new method that is flexible and controls the balance between false negatives and false positives for hit selection in RNA high-throughput screening assays. The author shows that the same decision rules and balances can be e...
Pharmacological characterization of purified recombinant mTOR FRB-kinase domain using fluorescence-based assays [0.03%]
基于荧光的分析技术纯化重组mTOR FRB-激酶结构域的药理学研究
Laurie J Reichling,Connie S Lebakken,Steven M Riddle et al.
Laurie J Reichling et al.
The mammalian target of rapamycin (mTOR) is a serine/threonine kinase involved in nutrient sensing and cell growth and is a validated target for oncology and immunosuppression. Two modes of direct small-molecule inhibition of mTOR activity ...
A profiling platform for the identification of selective metalloprotease inhibitors [0.03%]
一个用于识别选择性金属蛋白酶抑制剂的分析平台
Christophe Antczak,Constantin Radu,Hakim Djaballah
Christophe Antczak
Although proteases represent an estimated 5% to 10% of potential drug targets, inhibitors for metalloproteases (MPs) account for only a small proportion of all approved drugs, failures of which have typically been associated with lack of se...