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Related Experiment Video

Updated: Feb 6, 2026

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Applications of Reactive Cysteine Profiling.

Keriann M Backus1

  • 1Department of Biological Chemistry, University of California, Los Angeles, 615 Charles E. Young Dr South, BSRB, Room 350A, Los Angeles, CA, 90095, USA. kbackus@mednet.ucla.edu.

Current Topics in Microbiology and Immunology
|August 15, 2018
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Summary

Cysteine profiling reveals thousands of reactive cysteines for drug development. This approach identifies cysteine reactivity and accessibility, enabling the discovery of new covalent inhibitors and targeted therapies.

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Area of Science:

  • Biochemistry
  • Chemical Biology
  • Proteomics

Background:

  • Cysteine thiols are crucial in biological processes like catalysis and disulfide bond formation.
  • Cysteines are frequently modified and alkylated, making them key targets for drug and probe development.

Purpose of the Study:

  • To annotate cysteine reactivity, posttranslational modifications, and chemical probe accessibility.
  • To identify functional and targetable cysteines across the proteome.

Main Methods:

  • Quantitative proteomics
  • Activity-based protein profiling
  • High-throughput screening
  • Fragment-based ligand discovery

Main Results:

  • Thousands of functional and small-molecule targetable cysteines were identified across diverse proteins.
  • New cysteine-reactive electrophiles and compound libraries were synthesized.
  • Cysteine profiling enables unbiased identification of reactive cysteines.

Conclusions:

  • Cysteine profiling is a powerful strategy for developing potent and selective chemical probes.
  • This approach holds promise for the development of new covalent drugs.
  • Advancements in chemical proteomic strategies enhance cysteine identification and targeting.