Selective inhibition of plant serine hydrolases by agrochemicals revealed by competitive ABPP

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Selective inhibition of plant serine hydrolases by agrochemicals revealed by competitive ABPP.

Organophosphate and -phosphonates and their thio derivatives are often used in agroindustry as herbicides and insecticides, but their potential off-targets in the plant are poorly investigated. Here, we use competitive activity-based protein profiling (ABPP) of serine hydrolases (SHs) to detect targets of these agrochemicals and other compounds in Arabidopsis thaliana. Using broad-range and spe...

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Serine hydrolase inhibitors, which facilitate enzyme function assignment and are used to treat a range of human disorders, often act by an irreversible mechanism that involves covalent modification of the serine hydrolase catalytic nucleophile. The portion of mammalian serine hydrolases for which selective inhibitors have been developed, however, remains small. Here, we show that N-hydroxyhydan...

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The core of an enzyme molecule is its active site from the viewpoints of both academic research and industrial application. To reveal the structural and functional mechanism of an enzyme, one needs to know its active site; to conduct structure-based drug design by regulating the function of an enzyme, one needs to know the active site and its microenvironment as well. Given the atomic coordinat...

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ژورنال

عنوان ژورنال: Bioorganic & Medicinal Chemistry

سال: 2012

ISSN: 0968-0896

DOI: 10.1016/j.bmc.2011.06.040