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Updated: May 30, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Analysis of nuclear receptor acetylation
Chenguang Wang1, Michael Powell, Lifeng Tian
1Department of Stem Cell Biology and Regenerative Medicine, Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, PA 19107, USA. chenguang.wang@jefferson.edu
Protein acetylation, a key post-translational modification, regulates gene transcription and cellular processes. This chapter details methods for studying nuclear receptor (NR) acetylation and de-acetylation, highlighting potential challenges.
Area of Science:
- Biochemistry
- Molecular Biology
- Epigenetics
Background:
- Acetylation is a crucial post-translational modification involving the addition of an acetyl group to protein substrates.
- Histone acetylation, particularly at lysine residues, is linked to transcriptionally active chromatin, reducing DNA binding and enhancing transcription factor access.
- Beyond histones, acetylation regulates non-histone proteins, impacting cellular proliferation, survival, and intracellular trafficking.
Purpose of the Study:
- To detail protocols for investigating nuclear receptor (NR) acetylation and de-acetylation.
- To discuss potential pitfalls associated with NR acetylation and de-acetylation methodologies.
- To provide a comprehensive overview of studying NR post-translational modifications.
Main Methods:
- Focuses on established protocols for analyzing NR acetylation and de-acetylation.
- Describes techniques used in the characterization of NR acetylation.
- Includes discussion on potential experimental challenges and limitations.
Main Results:
- Acetylation of transcription factors, including nuclear receptors, can regulate cellular growth.
- Nuclear receptors possess a phylogenetically conserved motif for acetylation.
- Over a dozen nuclear receptors have been identified as substrates for acetyltransferases.
Conclusions:
- Nuclear receptor acetylation is a significant regulatory mechanism.
- Understanding NR acetylation and de-acetylation is vital for comprehending gene regulation.
- The chapter provides practical guidance and addresses methodological considerations for NR acetylation studies.
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