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Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
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Complex-specific inhibitors for interrogating ATAC histone acetyltransferase complex.
Sha Liu1, Jinzhao Liu2, Yinqiao Wu1
1Department of Chemistry, The University of Hong Kong, Hong Kong, China.
Nature Chemical Biology
|January 9, 2026
Summary
Researchers developed a chemical inhibitor targeting the YEATS2 subunit to specifically disrupt the ATAC (Ada-two-A-containing) histone acetyltransferase complex. This approach suppressed tumor growth by reducing ATAC complex activity and gene expression.
Area of Science:
- Biochemistry
- Molecular Biology
- Cancer Research
Background:
- Histone acetyltransferases (HATs) regulate gene expression through chromatin modification.
- HATs function in diverse protein complexes, influencing their specificity and function.
- Understanding complex-specific roles of HATs is crucial for targeted therapies.
Purpose of the Study:
- To develop a chemical method for specifically dissociating the ATAC HAT complex from chromatin.
- To investigate the therapeutic potential of inhibiting the ATAC complex in cancer.
Main Methods:
- Developed chemical inhibitors targeting YEATS2, a subunit specific to the ATAC complex.
- Utilized LS-170, a potent inhibitor, to reduce ATAC complex chromatin occupancy.
- Assessed the impact of ATAC complex inhibition on histone acetylation and gene expression.
Main Results:
- LS-170 specifically decreased ATAC complex binding to chromatin.
- Inhibition of the ATAC complex reduced histone acetylation levels.
- Downregulation of ATAC-governed genes led to suppressed tumor growth in a lung cancer model.
Conclusions:
- The ATAC HAT complex plays a significant role in gene transcription.
- Chemical inhibition of the ATAC complex is a viable therapeutic strategy for cancer treatment.
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