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Updated: May 21, 2026

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
05:33

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Published on: November 9, 2020

Discovery and Structural Optimization of BRD4-Selective Monovalent Direct Degraders

Geoffray Leriche1, Farhana Barmare1, Julia I Toth1

  • 1Plexium, 9330 Scranton Road, San Diego, California 92121, United States.

ACS Medicinal Chemistry Letters
|May 20, 2026
PubMed
Summary

Researchers discovered PLX-4104, a novel oral drug that selectively degrades the BRD4 protein. This targeted protein degradation approach shows promise for treating acute myeloid leukemia (AML) by causing complete tumor regression in models.

Keywords:
BRD4DCAF11medicinal chemistry optimizationmonovalent direct degradertargeted protein degradation

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