STA-55, an Easily Accessible, Broad-Spectrum, Activity-Based Aldehyde Dehydrogenase Probe
| Autor: | Sebastiaan T A Koenders, Bogdan I. Florea, Mario van der Stelt, Hans van den Elst, Herman S. Overkleeft, Eva J. van Rooden |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Proteomics
Aldehyde dehydrogenase 010402 general chemistry 01 natural sciences Biochemistry Downregulation and upregulation Cell Line Tumor medicine Humans Chemoproteomics Enzyme Inhibitors Molecular Biology Fluorescent Dyes chemistry.chemical_classification biology 010405 organic chemistry Chemistry Organic Chemistry Target engagement Activity-based proteomics Cancer Aldehyde Dehydrogenase medicine.disease 0104 chemical sciences Enzyme Drug Design biology.protein Molecular Medicine Click Chemistry |
| Zdroj: | CHEMBIOCHEM CHEMBIOCHEM, 21, 1911-1917. WILEY-V C H VERLAG GMBH |
| ISSN: | 1439-7633 |
| Popis: | Aldehyde dehydrogenases (ALDHs) convert aldehydes into carboxylic acids and are often upregulated in cancer. They have been linked to therapy resistance and are therefore potential therapeutic targets. However, only a few selective and potent inhibitors are currently available for this group of enzymes. Competitive activity-based protein profiling (ABPP) would aid the development and validation of new selective inhibitors. Herein, a broad-spectrum activity-based probe that reports on several ALDHs is presented. This probe was used in a competitive ABPP protocol against three ALDH inhibitors in lung cancer cells to determine their selectivity profiles and establish their target engagement. |
| Databáze: | OpenAIRE |
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