Development and Validation of a Universal High-Throughput UDP-Glycosyltransferase Assay with a Time-Resolved FRET Signal

2016 ◽  
Vol 14 (4) ◽  
pp. 240-251 ◽  
Author(s):  
Thomas Zielinski ◽  
Melvin Reichman ◽  
Preston S. Donover ◽  
Robert G. Lowery
Keyword(s):  
High Throughput ◽  
Time Resolved ◽  
Glycosyltransferase Assay ◽  
Development And Validation

Time-Resolved Luminescent High-Throughput Screening Platform for Lysosomotropic Compounds in Living Cells

ACS Sensors ◽  
2020 ◽  
Author(s):  
Ke-Jia Wu ◽  
Chun Wu ◽  
Feng Chen ◽  
Sha-Sha Cheng ◽  
Dik-Lung Ma ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Living Cells ◽  
Time Resolved ◽  
Screening Platform

scholarly journals High‐throughput dilution‐based growth method enables time‐resolved exo‐metabolomics of Pseudomonas putida and Pseudomonas aeruginosa

2021 ◽  
Author(s):  
Bjarke H. Pedersen ◽  
Nicolás Gurdo ◽  
Helle Krogh Johansen ◽  
Søren Molin ◽  
Pablo I. Nikel ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Pseudomonas Putida ◽  
High Throughput ◽  
Time Resolved ◽  
Growth Method

High-Throughput Screening to Identify Small Molecules That Selectively Inhibit APOL1 Protein Level in Podocytes

2021 ◽  
pp. 247255522110262
Author(s):  
Jonathan Choy ◽  
Yanqing Kan ◽  
Steve Cifelli ◽  
Josephine Johnson ◽  
Michelle Chen ◽  
...  
Keyword(s):  
Small Molecule ◽  
High Throughput ◽  
High Throughput Screening ◽  
Screening Strategy ◽  
Time Resolved ◽  
Protein Levels ◽  
Increased Risk ◽  
Compound Screening ◽  
High Throughput Screens ◽  
Screening Library

High-throughput phenotypic screening is a key driver for the identification of novel chemical matter in drug discovery for challenging targets, especially for those with an unclear mechanism of pathology. For toxic or gain-of-function proteins, small-molecule suppressors are a targeting/therapeutic strategy that has been successfully applied. As with other high-throughput screens, the screening strategy and proper assays are critical for successfully identifying selective suppressors of the target of interest. We executed a small-molecule suppressor screen to identify compounds that specifically reduce apolipoprotein L1 (APOL1) protein levels, a genetically validated target associated with increased risk of chronic kidney disease. To enable this study, we developed homogeneous time-resolved fluorescence (HTRF) assays to measure intracellular APOL1 and apolipoprotein L2 (APOL2) protein levels and miniaturized them to 1536-well format. The APOL1 HTRF assay served as the primary assay, and the APOL2 and a commercially available p53 HTRF assay were applied as counterscreens. Cell viability was also measured with CellTiter-Glo to assess the cytotoxicity of compounds. From a 310,000-compound screening library, we identified 1490 confirmed primary hits with 12 different profiles. One hundred fifty-three hits selectively reduced APOL1 in 786-O, a renal cell adenocarcinoma cell line. Thirty-one of these selective suppressors also reduced APOL1 levels in conditionally immortalized human podocytes. The activity and specificity of seven resynthesized compounds were validated in both 786-O and podocytes.

A high-throughput assay for HIV-1 integrase 3′-processing activity using time-resolved fluorescence

2012 ◽  
Vol 184 (1-2) ◽  
pp. 34-40 ◽  
Author(s):  
Ying-Shan Han ◽  
Peter Quashie ◽  
Thibault Mesplede ◽  
Hongtao Xu ◽  
Kevork Mekhssian ◽  
...  
Keyword(s):  
High Throughput ◽  
Time Resolved Fluorescence ◽  
Time Resolved ◽  
Processing Activity ◽  
High Throughput Assay ◽  
Hiv 1

scholarly journals The development and validation of EpiComet-Chip, a modified high-throughput comet assay for the assessment of DNA methylation status

2017 ◽  
Vol 58 (7) ◽  
pp. 508-521 ◽  
Author(s):  
Todd A. Townsend ◽  
Marcus C. Parrish ◽  
Bevin P. Engelward ◽  
Mugimane G. Manjanatha
Keyword(s):  
Dna Methylation ◽  
Comet Assay ◽  
High Throughput ◽  
Methylation Status ◽  
Development And Validation

scholarly journals Development and Validation of an Automated High-Throughput System for Zebrafish In Vivo Screenings

PLoS ONE ◽  
2012 ◽  
Vol 7 (5) ◽  
pp. e36690 ◽  
Author(s):  
Ainhoa Letamendia ◽  
Celia Quevedo ◽  
Izaskun Ibarbia ◽  
Juan M. Virto ◽  
Olaia Holgado ◽  
...  
Keyword(s):  
High Throughput ◽  
Development And Validation
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