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Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay
Karolinska Institute, Sweden .
Karolinska Institute, Sweden .
Karolinska Institute, Sweden .
Karolinska Institute, Sweden .
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2013 (English)In: Science, ISSN 0036-8075, E-ISSN 1095-9203, Vol. 341, no 6141, 84-87 p.Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
American Association for the Advancement of Science , 2013. Vol. 341, no 6141, 84-87 p.
National Category
Medical and Health Sciences
URN: urn:nbn:se:liu:diva-96173DOI: 10.1126/science.1233606ISI: 000321291700054OAI: diva2:640806
Available from: 2013-08-14 Created: 2013-08-14 Last updated: 2013-08-14

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Cao, Yihai
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Division of Cardiovascular MedicineFaculty of Health Sciences
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