Science· 2013Q1
Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay
- 2,232citations
- Q1SCImago
- 2013year
Short summary
The cellular thermal shift assay (CETSA) enables monitoring of drug binding to target proteins directly within cells and tissues, overcoming previous limitations in drug development.
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Key points
- Developed the cellular thermal shift assay (CETSA) to monitor drug-target binding in cells and tissues.
- CETSA is based on ligand-induced thermal stabilization of target proteins.
- Validated drug binding for clinical targets using CETSA.
- Monitored drug transport, activation, off-target effects, and resistance in cancer cell lines.
- Assessed drug distribution in tissues.
AI-generated from the title and abstract; the full text is not read.
Abstract
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.
The authors' abstract, as published at the source. Science, 2013 · DOI ↗
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Field: Computational Theory and Mathematics
Computational Theory and MathematicsComputer Science