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Activity-based proteomics: enzyme chemistry redux.

John W Kozarich1

  • 1ActivX Biosciences, 11025 North Torrey Pines Road, La Jolla, CA 92037, USA.

Current Opinion in Chemical Biology
|January 28, 2003
PubMed
Summary
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Activity-based probes are revolutionizing proteomics by enabling the study of enzyme activity in complex biological samples. This powerful new technology aids in identifying enzyme targets for drug discovery.

Area of Science:

  • Biochemistry
  • Proteomics
  • Chemical Biology

Background:

  • Enzyme chemistry, mechanism of action, and inhibitor design are foundational to understanding enzyme function.
  • Traditional proteomics methods often require extensive individual assay development and isolation for each enzyme.
  • The need exists for broader methods to interrogate enzyme activity in complex biological systems.

Purpose of the Study:

  • To introduce and elaborate on the application of activity-based probes in proteomics.
  • To highlight the potential of activity-based probes for interrogating enzyme family members, both known and unknown.
  • To underscore the value of this approach for drug discovery and development.

Main Methods:

  • Development and application of activity-based probes.

Related Experiment Videos

  • Utilizing principles of enzyme chemistry and inhibitor design.
  • Demonstration of proof-of-concept in serine hydrolases and cysteine proteases.

    • Main Results:

    • Activity-based probes offer a broad method for interrogating enzyme activity in cells and proteomic fractions.
    • This approach bypasses the need for individual enzyme assay development and isolation.
    • Serine hydrolases and cysteine proteases serve as successful examples, with other enzyme classes rapidly being explored.

    Conclusions:

    • Activity-based proteomics represents a significant advancement in the field.
    • This technology facilitates the study of enzyme function in native biological contexts.
    • The development of activity-based probes holds great promise for accelerating drug discovery and development efforts.