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

Bioorg Med Chem. 2012 Jan 15;20(2):597-600. doi: 10.1016/j.bmc.2011.06.040. Epub 2011 Jul 18.


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 specific probes, and by overexpression of various SHs in planta, we are able to confirm eight SH-compound interactions, including selective inhibition of carboxylesterase CXE12, prolyloligopeptidase, methylesterase MES2 and tripeptidyl peptidase TPP2. These observations can be used for the design of novel probes and selective inhibitors and may help to assess physiological effects of agrochemicals on crop plants.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Agrochemicals / chemistry*
  • Agrochemicals / pharmacology
  • Arabidopsis / enzymology
  • Herbicides / chemistry
  • Insecticides / chemistry
  • Organophosphates / chemistry
  • Plant Proteins / antagonists & inhibitors*
  • Plant Proteins / metabolism
  • Proteomics
  • Serine Proteases / chemistry*
  • Serine Proteases / metabolism
  • Serine Proteinase Inhibitors / chemistry*


  • Agrochemicals
  • Herbicides
  • Insecticides
  • Organophosphates
  • Plant Proteins
  • Serine Proteinase Inhibitors
  • Serine Proteases