ChemInform Abstract: A High-Content Screening Platform with Fluorescent Chemical Probes for the Discovery of First-in-Class Therapeutics

ChemInform ◽  
2016 ◽  
Vol 47 (30) ◽  
Author(s):  
Ala Jo ◽  
Jinjoo Jung ◽  
Eunha Kim ◽  
Seung Bum Park
Keyword(s):  
High Content Screening ◽  
Chemical Probes ◽  
Screening Platform

A high-content screening platform with fluorescent chemical probes for the discovery of first-in-class therapeutics

2016 ◽  
Vol 52 (47) ◽  
pp. 7433-7445 ◽  
Author(s):  
Ala Jo ◽  
Jinjoo Jung ◽  
Eunha Kim ◽  
Seung Bum Park
Keyword(s):  
Therapeutic Agents ◽  
High Content Screening ◽  
Phenotypic Screening ◽  
Chemical Probes ◽  
Screening Platform

Phenotypic screening as a promising approach to discover novel first-in-class therapeutic agents.

Predictive Modeling and Biomechanical Microengineering of Mesenchymal Stem Cells: A High Content Screening Platform to Enhance Lineage Specific Differentiation

2013 ◽  
Author(s):  
Amit Paul ◽  
David Franz ◽  
Sumaira Yahya ◽  
Shan Sun ◽  
Michael Cho
Keyword(s):  
Stem Cells ◽  
Mesenchymal Stem Cells ◽  
Stem Cell ◽  
Predictive Modeling ◽  
Stem Cell Differentiation ◽  
High Content Screening ◽  
Cell Behavior ◽  
Functional Changes ◽  
Screening Platform

Recent evidence suggests that stem cell differentiation can be regulated by modulation of the cell’s biomechanics. The cytoskeletal structures and arrangements in stem cells undergoing differentiation are dramatically altered, and these alterations vary by lineage. The complexity of events associated with the transformation of these precursor cells leaves many questions unanswered about morphological, structural, proteomic, and functional changes in differentiating stem cells. A thorough understanding of stem cell behavior, both experimentally and computationally, would allow for the development of more effective approaches to the expansion of stem cells in vitro and for the regulation of their commitment to a specific phenotype.

scholarly journals Activation and Translocation of Glucokinase in Rat Primary Hepatocytes Monitored by High Content Image Analysis

2008 ◽  
Vol 13 (9) ◽  
pp. 837-846 ◽  
Author(s):  
Michael Wolff ◽  
Stefan G. Kauschke ◽  
Susanne Schmidt ◽  
Ralf Heilker
Keyword(s):  
Regulatory Protein ◽  
Rat Hepatocytes ◽  
High Content Screening ◽  
Metabolic Enzyme ◽  
Screening Assay ◽  
Extracellular Medium ◽  
Rat Primary Hepatocytes ◽  
Translocation Assay ◽  
Low Glucose ◽  
Screening Platform

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 format to measure the nucleus-to-cytoplasm translocation of GK by reagents that destabilize the interaction between GK and GKRP. As a cellular model system, primary rat hepatocytes endogenously expressing both GK and GKRP at physiological levels were used. The GK translocation assay was robust, displayed limited day-to-day variability, and delivered good Z′ statistics. The increase of the glucose concentration in the extracellular medium from a low glucose situation (2.8 mM) to beyond its physiological set point value of 5 mM was found to drive GK from the nucleus into the cytoplasm. Likewise, both fructose (converted intracellularly into fructose-1-phosphate) and a known allosteric GK activator were found to induce the export of GK from the nucleus and to synergistically enhance the effects of medium or high glucose concentrations with respect to GK translocation. Transfer of the high content screening format to a semiautomated medium throughput screening platform enabled the profiling of large compound numbers with respect to allosteric activation of GK. ( Journal of Biomolecular Screening 2008:837-846)

scholarly journals A FRET-based high-throughput screening platform for the discovery of chemical probes targeting the scaffolding functions of human tankyrases

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Sven T. Sowa ◽  
Carlos Vela-Rodríguez ◽  
Albert Galera-Prat ◽  
Mariana Cázares-Olivera ◽  
Renata Prunskaite-Hyyryläinen ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Chemical Probes ◽  
Screening Platform
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