Pradeep Reddy Cingaram
Mol. Ther. Nucleic Acids, 2023, 33, 142-143
https://doi.org/10.1016/j.omtn.2023.06.014

Abstract

Epigenetic dysregulation plays a crucial role in the onset and progression of cancer, positioning them as compelling targets for therapeutic intervention. In a recent issue of Molecular Therapy – Nucleic Acids, Jeong et al. describe the identification of a novel selective bromodomain and extra-terminal motif (BET) inhibitor, BBC1115, using DNA-encoded library (DEL) screening.1 The study highlights the successful application of DEL-based small-molecule compound screening coupled with intensive biological characterization to discover new chemotypes with selectivity, efficacy, and safety profiles for targeting proteins involved in epigenetic regulation in human malignancies.