The GFP thermal shift assay for screening ligand and lipid interactions to solute carrier transporters

2021 ◽  
Author(s):  
Yurie Chatzikyriakidou ◽  
Do-Hwan Ahn ◽  
Emmanuel Nji ◽  
David Drew
Keyword(s):  
Lipid Interactions ◽  
Thermal Shift Assay ◽  
Solute Carrier Transporters ◽  
Solute Carrier ◽  
Thermal Shift

scholarly journals Detection of Chemical Engagement of Solute Carrier Proteins by a Cellular Thermal Shift Assay

2018 ◽  
Vol 13 (6) ◽  
pp. 1480-1486 ◽  
Author(s):  
Mari Hashimoto ◽  
Enrico Girardi ◽  
Ruth Eichner ◽  
Giulio Superti-Furga
Keyword(s):  
Carrier Proteins ◽  
Thermal Shift Assay ◽  
Solute Carrier ◽  
Cellular Thermal Shift Assay ◽  
Thermal Shift

Rapid Evaluation of Small Molecule Cellular Target Engagement with a Luminescent Thermal Shift Assay

2021 ◽  
Author(s):  
Jonathan D. Mortison ◽  
Ivan Cornella-Taracido ◽  
Gireedhar Venkatchalam ◽  
Anthony W. Partridge ◽  
Nirodhini Siriwardana ◽  
...  
Keyword(s):  
Small Molecule ◽  
Rapid Evaluation ◽  
Target Engagement ◽  
Thermal Shift Assay ◽  
Cellular Target ◽  
Thermal Shift

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

Science ◽  
2013 ◽  
Vol 341 (6141) ◽  
pp. 84-87 ◽  
Author(s):  
Daniel Martinez Molina ◽  
Rozbeh Jafari ◽  
Marina Ignatushchenko ◽  
Takahiro Seki ◽  
E. Andreas Larsson ◽  
...  
Keyword(s):  
Drug Target ◽  
Drug Transport ◽  
Drug Binding ◽  
Target Engagement ◽  
Tissue Samples ◽  
Target Proteins ◽  
Thermal Shift Assay ◽  
Cellular Thermal Shift Assay ◽  
Thermal Shift ◽  
In Cells

The efficacy of therapeutics is dependent on a drug binding to its cognate target. Optimization of target engagement by drugs in cells is often challenging, because drug binding cannot be monitored inside cells. We have developed a method for evaluating drug binding to target proteins in cells and tissue samples. This cellular thermal shift assay (CETSA) is based on the biophysical principle of ligand-induced thermal stabilization of target proteins. Using this assay, we validated drug binding for a set of important clinical targets and monitored processes of drug transport and activation, off-target effects and drug resistance in cancer cell lines, as well as drug distribution in tissues. CETSA is likely to become a valuable tool for the validation and optimization of drug target engagement.

Sign in / Sign up

Export Citation Format

Share Document