ArticlePloS one2018
A high content, high throughput cellular thermal stability assay for measuring drug-target engagement in living cells.
Article in PloS one, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 32 citations in OpenAlex.
- Thermal shift engagement assay for Class IIA histone deacetylase inhibitor screening.Results in chemistry · 2025Article
- Dopamine modification of glycolytic enzymes impairs glycolysis: possible implications for Parkinson's disease.Cell communication and signaling : CCS · 2024Article
- Thermal unfolding methods in drug discovery.Biophysics reviews · 2023Review
- Monitoring drug-target interactions through target engagement-mediated amplification on arrays and in situ.Nucleic acids research · 2022Article
- Real-Time Cellular Thermal Shift Assay to Monitor Target Engagement.ACS chemical biology · 2022Article
- Organelle specific fluorescent phenomics and transcriptomic profiling to evaluate cellular response to tris(1,3 dichloro 2 propyl)phosphate.Scientific reports · 2022Article
- High-Throughput Cellular Thermal Shift Assay Using Acoustic Transfer of Protein Lysates.ACS chemical biology · 2022Article
- Current Advances in CETSA.Frontiers in molecular biosciences · 2022Review
- An update of label-free protein target identification methods for natural active products.Theranostics · 2022Review
- A Review of In Vitro Instrumentation Platforms for Evaluating Thermal Therapies in Experimental Cell Culture Models.Critical reviews in biomedical engineering · 2022Review
- High-Throughput Cellular Thermal Shift Assays in Research and Drug Discovery.SLAS discovery : advancing life sciences R & D · 2020Article
- CETSA-based target engagement of taxanes as biomarkers for efficacy and resistance.Scientific reports · 2019Article
- Positioning High-Throughput CETSA in Early Drug Discovery through Screening against B-Raf and PARP1.SLAS discovery : advancing life sciences R & D · 2019Article
Corrections and comments
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Authors and funding
1 author at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Determining and understanding drug target engagement is critical for drug discovery. This can be challenging within living cells as selective readouts are often unavailable. Here we describe a novel method for measuring target engagement in living cells based on the principle of altered protein thermal stabilization / destabilization in response to ligand binding. This assay (HCIF-CETSA) utilizes high content, high throughput single cell immunofluorescent detection to determine target protein levels following heating of adherent cells in a 96 well plate format. We have used target engagement of Chk1 by potent small molecule inhibitors to validate the assay. Target engagement measured by this method was subsequently compared to target engagement measured by two alternative methods (autophosphorylation and CETSA). The HCIF-CETSA method appeared robust and a good correlation in target engagement measured by this method and CETSA for the selective Chk1 inhibitor V158411 was observed. However, these EC50 values were 23- and 12-fold greater than the autophosphorylation IC50. The described method is therefore a valuable advance in the CETSA method allowing the high throughput determination of target engagement in adherent cells.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.