Journal
SCIENCE
Volume 341, Issue 6141, Pages 84-87Publisher
AMER ASSOC ADVANCEMENT SCIENCE
DOI: 10.1126/science.1233606
Keywords
-
Categories
Funding
- KI (Distinguished Professor Award)
- Swedish Research Council (Vetenskapsradet)
- Swedish Cancer Society (Cancerfonden)
- Strategic Centre grant from Nanyang Technological University (Singapore)
- Karolinska Institute Foundation
- Torsten Soderbergs Foundation
- European Research Council [250021]
- European Research Council (ERC) [250021] Funding Source: European Research Council (ERC)
Ask authors/readers for more resources
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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available