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Related Experiment Video

Updated: Apr 28, 2026

Screening Traditional Chinese Medicine Compounds for Inhibiting UCHL3 Activity Based on Molecular Docking and Deubiquitinating Enzyme Probe Technology
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Enzyme inhibitor discovery by activity-based protein profiling.

Micah J Niphakis1, Benjamin F Cravatt

  • 1The Skaggs Institute for Chemical Biology and the Department of Chemical Physiology, The Scripps Research Institute, La Jolla, California 92037;

Annual Review of Biochemistry
|June 7, 2014
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Summary

Activity-based protein profiling (ABPP) discovers selective enzyme inhibitors. These chemical probes reveal enzyme functions, uncovering pathways crucial for human health and disease.

Keywords:
activity-based protein profilingchemical proteomicsenzymeinhibitortarget engagement

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Area of Science:

  • Biochemistry
  • Chemical Biology
  • Proteomics

Background:

  • Many enzymes in eukaryotic and prokaryotic organisms remain uncharacterized.
  • Selective inhibitors are essential tools for probing enzyme functions in biological systems.

Purpose of the Study:

  • To discuss the application of activity-based protein profiling (ABPP) for discovering selective, in vivo-active enzyme inhibitors.
  • To highlight the use of these inhibitors in elucidating enzyme functions and biological pathways.

Main Methods:

  • Utilizing the chemical proteomic platform, activity-based protein profiling (ABPP).
  • Developing selective and in vivo-active enzyme inhibitors.
  • Employing inhibitors to delineate biochemical and cellular enzyme functions.

Main Results:

  • Discovery of selective inhibitors for uncharacterized enzymes.
  • Identification of novel metabolic and signaling pathways.
  • Elucidation of enzyme roles in human physiology and disease.

Conclusions:

  • Activity-based protein profiling (ABPP) is a powerful method for enzyme inhibitor discovery.
  • Selective chemical probes are valuable tools for advancing biological research.
  • This approach facilitates the discovery of pathways critical to human health and disease.