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The cellular thermal shift assay for evaluating drug target interactions in cells
Thermal shift assays are used to study thermal stabilization of proteins upon ligand binding. Such assays have been used extensively on purified proteins in the drug discovery industry and inExpand
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CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil
Target engagement is a critical factor for therapeutic efficacy. Assessment of compound binding to native target proteins in live cells is therefore highly desirable in all stages of drug discovery.Expand
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Targeted NUDT5 inhibitors block hormone signaling in breast cancer cells
With a diverse network of substrates, NUDIX hydrolases have emerged as a key family of nucleotide-metabolizing enzymes. NUDT5 (also called NUDIX5) has been implicated in ADP-ribose and 8-oxo-guanineExpand
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Organic Hazardous Substances in Graywater from Swedish Households
The concentrations of several selected organic hazardous substances were investigated in domestic graywater. In total, 41 of 81 organic hazardous substances were found in concentrations above theExpand
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Screening for Target Engagement using the Cellular Thermal Shift Assay - CETSA
TLDR
The direct measurement of drug-protein interactions in living cells is a major challenge in drug discovery research. Expand
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Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery
Significance Exposure at the site of action has been identified as one of the three most important factors for success in drug discovery and the design of chemical probes. Modern drug discoveryExpand
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Inhibitors of the Cysteine Synthase CysM with Antibacterial Potency against Dormant Mycobacterium tuberculosis.
Cysteine is an important amino acid in the redox defense of Mycobacterium tuberculosis, primarily as a building block of mycothiol. Genetic studies have implicated de novo cysteine biosynthesis inExpand
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In Situ Target Engagement Studies in Adherent Cells.
A prerequisite for successful drugs is effective binding of the desired target protein in the complex environment of a living system. Drug-target engagement has typically been difficult to monitor inExpand
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The Use of TrkA-PathHunter Assay in High-Throughput Screening to Identify Compounds That Affect Nerve Growth Factor Signaling
The TrkA-PathHunter cell-based assay was used in high-throughput screening (HTS) to identify compounds that inhibit nerve growth factor (NGF)/TrkA signaling. The assay was conducted in a 384-wellExpand
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