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Updated: May 15, 2026

An Acetyl-Click Chemistry Assay to Measure Histone Acetyltransferase 1 Acetylation
Published on: January 26, 2024
Cancers with wrong HATs: the impact of acetylation
Vincenzo Di Cerbo1, Robert Schneider
1Max-Planck Institute of Immunobiology and Epigenetics in Freiburg, Germany.
Abstract:
Lysine N-ε-acetylation is a post-translational modification that regulates the function of histone and non-histone proteins. In several malignancies, histone acetyltransferase (HAT) activities are disturbed as a consequence of various genetic or epigenetic alterations. In particular, HATs can function as tumor suppressors, helping cells control cellular proliferation and cell cycle, and also as oncogenes, because abnormal acetylation can activate malignant proteins and contribute to cancer. An impaired acetylation profile can be indicative of a pathological process, and thus evaluation of histone acetylation could be used as a predictive index of patient survival or therapy outcome. Therefore, epigenetic therapy might be a very effective strategy to defeat cancer. With the use of histone deacetylase inhibitors and acetylation modulators (e.g. HAT inhibitors, bromodomain inhibitors), we are paving the way for a future epigenetic drug control of human diseases.
Insights
Lysine acetylation regulates protein function and is crucial in cancer development. Evaluating histone acetylation may predict patient outcomes and guide epigenetic therapy for cancer treatment.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Lysine N-ε-acetylation is a key post-translational modification regulating histone and non-histone protein functions.
- Dysregulated histone acetyltransferase (HAT) activity, due to genetic or epigenetic changes, is implicated in various malignancies.
- Altered acetylation profiles can indicate pathological processes and serve as predictive biomarkers for patient survival and therapy response.
Purpose of the Study:
- To explore the role of lysine acetylation in cancer.
- To highlight the potential of histone acetylation evaluation as a predictive index.
- To emphasize the promise of epigenetic therapy in cancer treatment.
Main Methods:
- Review of literature on lysine acetylation, HATs, and epigenetic alterations in cancer.
- Analysis of the dual role of HATs as tumor suppressors and oncogenes.
- Discussion of therapeutic strategies targeting acetylation pathways.
Main Results:
- Histone acetylation status is altered in malignancies, impacting cellular proliferation and cell cycle control.
- Abnormal acetylation can activate oncogenic proteins, contributing to cancer progression.
- Histone acetylation evaluation shows potential as a predictive biomarker for patient outcomes.
Conclusions:
- Epigenetic modifications, particularly lysine acetylation, are critical in cancer pathogenesis.
- Targeting acetylation pathways with epigenetic drugs, such as HAT inhibitors and bromodomain inhibitors, offers a promising therapeutic strategy.
- Epigenetic therapy holds significant potential for controlling human diseases, including cancer.
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