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Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with

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Researchers developed potent small-molecule inhibitors targeting p300/CBP histone acetyltransferases (HATs). These inhibitors, particularly fluorinated compound 22, show promise in reducing Myc expression and improving pharmacokinetic properties for potential therapeutic applications.

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Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Molecular Biology

Background:

  • p300/CBP are homologous histone acetyltransferases crucial for cellular processes.
  • Dysregulation of p300/CBP is implicated in various diseases, including cancer.
  • Inhibition of p300/CBP can reduce Myc expression, a key oncogene.

Purpose of the Study:

  • To identify potent small-molecule inhibitors of p300/CBP HATs.
  • To optimize inhibitor pharmacokinetic properties through strategies like reducing ChromlogD and fluorination.
  • To evaluate the impact of these inhibitors on cMyc cellular potency.

Main Methods:

  • Utilized DNA-encoded library technology for inhibitor discovery.
  • Employed high-throughput screening to identify potent compounds.
  • Applied medicinal chemistry strategies, including fluorination and ChromlogD reduction, for optimization.

Main Results:

  • Identified a series of potent, proline-based small-molecule p300/CBP HAT inhibitors.
  • Developed compound 22 with improved pharmacokinetic properties.
  • Demonstrated that fluorination of compound 22 reduced clearance and enhanced cMyc cellular potency.

Conclusions:

  • The identified inhibitors represent promising leads for therapeutic intervention in diseases involving p300/CBP dysregulation.
  • Medicinal chemistry strategies, particularly fluorination, are effective in enhancing the drug-like properties of p300 inhibitors.
  • Targeting p300/CBP with optimized small molecules offers a viable strategy for modulating Myc expression in cancer and other diseases.