2. Academic Validation
  3. The GCN5: its biological functions and therapeutic potentials

The GCN5: its biological functions and therapeutic potentials

  • Clin Sci (Lond). 2021 Jan 15;135(1):231-257. doi: 10.1042/CS20200986.
Md Ezazul Haque 1,  Md Jakaria 1,  Mahbuba Akther 1,  Duk-Yeon Cho 1,  In-Su Kim 2,  Dong-Kug Choi 1 2
Affiliations

Affiliations

  • 1 Department of Applied Life Science, Graduate School, BK21 Program, Konkuk University, Chungju 27478, Republic of Korea.
  • 2 Department of Biotechnology, College of Biomedical and Health Science, and Research Institute of Inflammatory Disease (RID), Konkuk University, Chungju 27478, Republic of Korea.
PMID: 33443284 DOI: 10.1042/CS20200986
Abstract

General control non-depressible 5 (GCN5) or lysine acetyltransferase 2A (KAT2A) is one of the most highly studied histone acetyltransferases. It acts as both Histone Acetyltransferase (HAT) and lysine acetyltransferase (KAT). As an HAT it plays a pivotal role in the epigenetic landscape and chromatin modification. Besides, GCN5 regulates a wide range of biological events such as gene regulation, cellular proliferation, metabolism and inflammation. Imbalance in the GCN5 activity has been reported in many disorders such as Cancer, metabolic disorders, autoimmune disorders and neurological disorders. Therefore, unravelling the role of GCN5 in different diseases progression is a prerequisite for both understanding and developing novel therapeutic agents of these diseases. In this review, we have discussed the structural features, the biological function of GCN5 and the mechanical link with the diseases associated with its imbalance. Moreover, the present GCN5 modulators and their limitations will be presented in a medicinal chemistry perspective.

Keywords

GCN5; Histone Acetyltransferase; Therapeutic implications; Transcriptional Regulation.

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