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Related Concept Videos

Covalently Linked Protein Regulators02:04

Covalently Linked Protein Regulators

Proteins can undergo many types of post-translational modifications, often in response to changes in their environment. These modifications play an important role in the function and stability of these proteins. Covalently linked molecules include functional groups, such as methyl, acetyl, and phosphate groups, and also small proteins, such as ubiquitin. There are around 200 different types of covalent regulators that have been identified.
These groups modify specific amino acids in a protein.

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Development of a Lysine-Reactive Targeted Covalent Inhibitor for the P300/CBP-Associated Factor Bromodomain Through

Richard R Ede1, Kerstin E Peterson1, Richard K Begyinah2

  • 1Department of Chemistry, University of Minnesota, Minneapolis, Minnesota, USA.

Chemmedchem
|May 22, 2026
PubMed
Summary

Researchers developed the first covalent inhibitor for the epigenetic regulatory protein PCAF (P300/CBP-associated factor). This new molecule targets PCAF effectively, offering a promising avenue for developing novel cancer therapies.

Keywords:
KAT2Bcovalent inhibitorsdrug discoverylysine‐reactivep300/CBP‐associated factor

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Area of Science:

  • Epigenetics
  • Molecular Biology
  • Drug Discovery

Background:

  • P300/CBP-associated factor (PCAF) is a key epigenetic regulator involved in HIV-1 transcription and glioblastoma.
  • Existing PCAF inhibitors are non-covalent and require high concentrations.
  • A novel covalent inhibition strategy is explored to overcome limitations of current treatments.

Purpose of the Study:

  • To design and develop novel covalent inhibitors targeting PCAF.
  • To investigate the mechanism of action and efficacy of these inhibitors.
  • To establish a foundation for future PCAF-targeted therapeutics.

Main Methods:

  • Rational design of lysine-reactive molecules based on a lead scaffold.
  • Evaluation of inhibition, selectivity, and kinetics using mass spectrometry.
  • Biophysical and cellular assays to confirm covalent mechanism and in-cell target engagement.

Main Results:

  • Development of the first covalent PCAF inhibitor, compound 10.
  • Compound 10 demonstrated covalent labeling of PCAF in vitro.
  • Verified in-cell engagement and covalent mechanism of compound 10.

Conclusions:

  • The first covalent PCAF inhibitor was successfully developed.
  • Compound 10 shows potential for future optimization and development of heterobifunctional molecules.
  • This study provides a new strategy for targeting PCAF in epigenetic regulation and disease.