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Published on: December 7, 2017
A bivalent role of TIP60 histone acetyl transferase in human cancer
Gaëlle Judes1,2, Khaldoun Rifaï1,2, Marjolaine Ngollo1,2
1Department of Oncogenetics, Centre Jean Perrin, CBRV, 28 place Henri Dunant, 63001 Clermont-Ferrand, France.
Abstract:
Acetylation is a major modification that is required for gene regulation, genome maintenance and metabolism. A dysfunctional acetylation plays an important role in several diseases, including cancer. A group of enzymes-lysine acetyltransferases are responsible for this modification and act in regulation of transcription as cofactors and by acetylation of histones and other proteins. Tip60, a member of MYST family, is expressed ubiquitously and is the acetyltransferase catalytic subunit of human NuA4 complex. This HAT has a well-characterized involvement in many processes, such as cellular signaling, DNA damage repair, transcriptional and cellular cycle. Aberrant lysine acetyltransferase functions promote or suppress tumorigenesis in different cancers such as colon, breast and prostate tumors. Therefore, Tip60 might be a potential and important therapeutic target in the cancer treatment; new histone acetyl transferase inhibitors were identified and are more selective inhibitors of Tip60.
Insights
Lysine acetyltransferases regulate gene expression and metabolism. Dysfunctional acetylation, particularly involving Tip60, is implicated in cancer, making Tip60 a potential therapeutic target.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Acetylation is a crucial post-translational modification regulating gene expression, genome stability, and metabolism.
- Lysine acetyltransferases (KATs) are enzymes responsible for acetylation, impacting transcription, DNA repair, and cell cycle.
- Dysfunctional acetylation is linked to various diseases, notably cancer, highlighting the importance of KATs in tumorigenesis.
Purpose of the Study:
- To investigate the role of the lysine acetyltransferase Tip60 in cellular processes and its implication in cancer.
- To explore Tip60 as a potential therapeutic target for cancer treatment.
- To identify and characterize novel, selective inhibitors of Tip60.
Main Methods:
- Characterization of Tip60's enzymatic activity and cellular functions.
- Analysis of Tip60's involvement in DNA damage repair and transcriptional regulation.
- Screening and validation of new histone acetyltransferase (HAT) inhibitors targeting Tip60.
Main Results:
- Tip60, a component of the NuA4 complex, is ubiquitously expressed and involved in critical cellular functions.
- Aberrant KAT activity, including Tip60, is associated with the promotion or suppression of tumorigenesis in various cancers.
- Development of novel, selective Tip60 inhibitors has been achieved.
Conclusions:
- Tip60 plays a significant role in cellular regulation and is implicated in cancer development.
- Tip60 represents a promising therapeutic target for anticancer strategies.
- Selective Tip60 inhibitors offer a potential avenue for targeted cancer therapy.
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