ReviewFrontiers in molecular biosciences2022
Current Advances in CETSA.
Review in Frontiers in molecular biosciences, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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Who cites it
39 citing papers in PubMed.
- Neoliensinine promotes lysosomal cell death in T cell malignancies via a novel STING-TUBA1B pathway.Genes & diseases · 2026Article
- Closing the Translational Gap: Closed-Loop AI Discovery Frameworks for Experimental Validation and Clinical Implementation in Cancer Therapeutics.Cancer medicine · 2026Review
- Recent advances in proteomic strategies for target identification of traditional Chinese medicine.Journal of pharmaceutical analysis · 2026Review
- Nobiletin attenuates LPS-induced acute lung injury via a STING-dependent signaling pathway.Archives of pharmacal research · 2026Article
- Progress and application of activity-based protein profiling for the discovery of natural product targets.Molecular diversity · 2026Review
- How Polyphenol Metabolites Spatiotemporally Reprogram Transcription Factors and Human Proteostasis: A Metabolite-Centric Framework.Current issues in molecular biology · 2026Review
- Optimization and Characterization of SHIP1 Ligands for Cellular Target Engagement and Activity in Alzheimer's Disease Models.Journal of medicinal chemistry · 2026Article
- AI and network biology for rational polypharmacology in signaling drug design: a review.NPJ precision oncology · 2026Review
- Lipo-Glc-1,6-PIUBMB life · 2026Article
- Rosmarinic Acid Targets AKR1B1 to Ameliorate Atherosclerosis via Vascular Endothelial Cell Energy Metabolism Regulation.Biomolecules · 2026Article
- Optimization and Characterization of SHIP1 Ligands for Cellular Target Engagement and Activity in Alzheimer's Disease Models.bioRxiv : the preprint server for biology · 2026Article
- High-throughput screening for biostimulant discovery: opportunities to enhance nitrogen use efficiency.Frontiers in plant science · 2026Review
- Small-molecule probes based on natural products: Elucidation of drug-target mechanisms in stroke.Journal of pharmaceutical analysis · 2025Review
- Ginsenoside Rc mitigates hippocampal neuronal damage and cognitive impairment in vascular dementia rats via the pY705-Stat3/Foxo3a and pS727-Stat3/GRIM-19 pathways.Journal of ginseng research · 2025Article
- Mechanisms that matter: unbiased cellular screening for degraders.npj drug discovery · 2025Review
- Covalent Degraders of Immune Regulatory Transcription Factors IRF8 and IRF5.bioRxiv : the preprint server for biology · 2025Article
- Elaboration of molecular glues that target TRIM21 into TRIMTACs that degrade protein aggregates.Nature communications · 2025Article
- Applications of the Cellular Thermal Shift Assay to Drug Discovery in Natural Products: A Review.International journal of molecular sciences · 2025Review
- MAST Kinases' Function and Regulation: Insights from Structural Modeling and Disease Mutations.Biomedicines · 2025Article
- Trifluridine/tipiracil induces ferroptosis by targeting p53 via the p53-SLC7A11 axis in colorectal cancer 3D organoids.Cell death & disease · 2025Article
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Funding
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Abstract
Knowing that the drug candidate binds to its intended target is a vital part of drug discovery. Thus, several labeled and label-free methods have been developed to study target engagement. In recent years, the cellular thermal shift assay (CETSA) with its variations has been widely adapted to drug discovery workflows. Western blot-based CETSA is used primarily to validate the target binding of a molecule to its target protein whereas CETSA based on bead chemistry detection methods (CETSA HT) has been used to screen molecular libraries to find novel molecules binding to a pre-determined target. Mass spectrometry-based CETSA also known as thermal proteome profiling (TPP) has emerged as a powerful tool for target deconvolution and finding novel binding partners for old and novel molecules. With this technology, it is possible to probe thermal shifts among over 7,000 proteins from one sample and to identify the wanted target binding but also binding to unwanted off-targets known to cause adverse effects. In addition, this proteome-wide method can provide information on the biological process initiated by the ligand binding. The continued development of mass spectrometry labeling reagents, such as isobaric tandem mass tag technology (TMT) continues to increase the throughput of CETSA MS, allowing its use for structure-activity relationship (SAR) studies with a limited number of molecules. In this review, we discussed the differences between different label-free methods to study target engagement, but our focus was on CETSA and recent advances in the CETSA method.
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