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STA‐55, an Easily Accessible, Broad‐Spectrum, Activity‐Based Aldehyde Dehydrogenase Probe
Author(s) -
Koenders Sebastiaan T. A.,
Rooden Eva J.,
Elst Hans,
Florea Bogdan I.,
Overkleeft Herman S.,
Stelt Mario
Publication year - 2020
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201900771
Subject(s) - aldehyde dehydrogenase , aldehyde , enzyme , broad spectrum , chemistry , combinatorial chemistry , biochemistry , computational biology , cancer research , biology , catalysis
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.