Extraction, identification, and functional characterization of a bioactive substance from automated compound-handling plastic tips [0.03%]
自动化化合物处理塑料吸头中生物活性物质的提取、鉴定和功能表征
John Watson,Emily B Greenough,John E Leet et al.
John Watson et al.
Disposable plastic labware is ubiquitous in contemporary pharmaceutical research laboratories. Plastic labware is routinely used for chemical compound storage and during automated liquid-handling processes that support assay development, hi...
Use of a real-time fluorescence monitoring system for high-throughput screening for prolyl isomerase inhibitors [0.03%]
用于脯氨酰异构酶抑制剂高通量筛选的实时荧光监测系统的方法学研究
Tadashi Mori,Seima Itami,Tomotaka Yanagi et al.
Tadashi Mori et al.
Cyclophilin is a ubiquitous peptidyl prolyl cis/trans isomerase that plays critical roles in many biological processes. A number of cyclophilin inhibitors have been designed based on the structure of the immunosuppressant cyclosporin A. To ...
New high-throughput fluorimetric assay for discovering inhibitors of UDP-N-acetylmuramyl-L-alanine: D-glutamate (MurD) ligase [0.03%]
一种用于发现UDP-N-乙酰胞壁酸-(甘氨酸磷酸转氨酶底物类似物的新型高通量荧光检测方法
Katja Kristan,Miha Kotnik,Marko Oblak et al.
Katja Kristan et al.
A novel assay for monitoring the activity of the bacterial enzyme UDP-N-acetylmuramyl-L-alanine:D-glutamate ligase (MurD ligase) is presented. MurD, which belongs to an enzyme family of Mur ligases, is essential for the synthesis of bacteri...
Development of a cell-based assay for measurement of c-Met phosphorylation using AlphaScreen technology and high-content imaging analysis [0.03%]
基于细胞的c-Met磷酸化检测分析方法的建立及评价
Nadya Smotrov,Anjili Mathur,Ilona Kariv et al.
Nadya Smotrov et al.
c-Met is a receptor tyrosine kinase (RTK) with a critical role in many fundamental cellular processes, including cell proliferation and differentiation. Deregulated c-Met signaling has been implicated in both the initiation and progression ...
Screening for NNRTIs with slow dissociation and high affinity for a panel of HIV-1 RT variants [0.03%]
用于HIV-1逆转录酶变异体筛选慢解离高亲和力非核苷类反转 transcriptase 抑制剂的试验体系
Malin Elinder,Helena Nordström,Matthis Geitmann et al.
Malin Elinder et al.
A lead optimization library consisting of 800 HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) was screened in parallel against 4 clinically relevant variants of HIV-1 RT (Wt, L100I, Y181C, and K103N) using a surface plasmon re...
Kappa opioid receptor screen with the Tango beta-arrestin recruitment technology and characterization of hits with second-messenger assays [0.03%]
采用 Tango β- arrestin 募集技术进行卡塔痛受体筛选及活性确证
Christopher Doucette,Kevin Vedvik,Elizabeth Koepnick et al.
Christopher Doucette et al.
Assays for high-throughput screening of G-protein-coupled receptors (GPCRs) have typically revolved around receptor binding, guanine nucleotide binding, and second-messenger assays measuring intracellular cAMP and calcium levels. New assay ...
Beta-arrestin-based Bret2 screening assay for the "non"-beta-arrestin binding CB1 receptor [0.03%]
基于β-arrestin的Bret2筛选检测CB1受体的“非”β-arrestin结合力
Milka Vrecl,Pia Karina Nørregaard,Dorthe L C Almholt et al.
Milka Vrecl et al.
CB1 receptor (CB1R) antagonists have been demonstrated to be effective in treating obesity and related disorders. This study has been focused on establishing a beta-arrestin 2-based screening assay for the CB1R using BRET2 technology. When ...
Design, synthesis, and pharmacology of fluorescently labeled analogs of serotonin: application to screening of the 5-HT2C receptor [0.03%]
荧光素标记的血清素类似物的设计、合成及药理学特性研究及其在五-羟色胺2c（5-HT2C）受体筛选中的应用
Peter Cornelius,Eunsun Lee,Wen Lin et al.
Peter Cornelius et al.
Novel fluorescent derivatives of serotonin have been synthesized and used as tracers for the development of a 5-HT2C fluorescence polarization assay. Serotonin analogs that feature a fluorescent probe attached through an ether linkage at th...
The interaction of proline-rich ligands with profilin probed with an enzyme-linked immunosorbent assay [0.03%]
采用酶联免疫吸附法探索富含脯氨酸配体与profilin的相互作用
Sylvie Veniere,Christophe Ampe,Joël Vandekerckhove et al.
Sylvie Veniere et al.
To detect interactions of different proline-rich ligands with profilins, the authors developed a simple analytical antibody-based screening method. Profilin I or profilin IIa was coated in microplates, and ligand binding was monitored via a...
Samantha Perspicace,David Banner,Jörg Benz et al.
Samantha Perspicace et al.
Surface plasmon resonance (SPR) technology has emerged as a new and powerful technique to investigate the interaction between low-molecular-weight molecules and target proteins. In the present work, the authors assemble from a large compoun...