Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay
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Summary
This cellular thermal shift assay (CETSA) is based on the biophysical principle of ligand-induced thermal stabilization of target proteins and 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.
- Type
- article
- Published
- 2013-07-05
- Cited by
- 1,988
- References
- 41
- OpenAlex
- https://openalex.org/W1993251792
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:5225262
Keywords
Drug, Drug resistance, Drug target, Plasma protein binding, Chemistry
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- Phase I dose escalation pharmacokinetics of O-(chloroacetylcarbamoyl) fumagillol (TNP-470) and its metabolites in AIDS patients with Kaposi's sarcoma
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- Biophysics in drug discovery: impact, challenges and opportunities
- Affinity-Based Selectivity Profiling of an In-Class Selective Competitive Inhibitor of Acyl Protein Thioesterase 2.
- Polypharmacology by Design: A Medicinal Chemist's Perspective on Multitargeting Compounds.
- A Guide to Run Affinity Screens Using Differential Scanning Fluorimetry and Surface Plasmon Resonance Assays.
- Development of allosteric and selective CDK2 inhibitors for contraception with negative cooperativity to cyclin binding
- Drug Affinity Responsive Target Stability (DARTS) for Small Molecule Target Identification
- A cellular screen identifies ponatinib and pazopanib as inhibitors of necroptosis
- Global analysis of protein folding thermodynamics for disease state characterization and biomarker discovery
- Hide and seek: Identification and confirmation of small molecule protein targets.
- Advances in measuring single-cell pharmacokinetics and pharmacology in vivo
- Novel Small Molecule Inhibitors for the Human Kinesins Mklp2 and Kif18A
- Discovery of Novel Inhibitors and Fluorescent Probe Targeting NAMPT
- Application of chemical biology in target identification and drug discovery
- The promise and peril of chemical probes
- Lost in Translation (LiT)
- Identification of a new class of natural product MDM2 inhibitor: In vitro and in vivo anti-breast cancer activities and target validation
- Hsp90 Is a Novel Target Molecule of CDDO-Me in Inhibiting Proliferation of Ovarian Cancer Cells
- A global map of lipid-binding proteins and their ligandability in cells
- Assessing the Efficacy of Mdm2/Mdm4-Inhibiting Stapled Peptides Using Cellular Thermal Shift Assays
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