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Targeting KAT6A/B as a New Therapeutic Strategy for Cancer Therapy
Tianpeng Zheng1, Shanglong Wang1, Wukun Liu1
1Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, School of Medicine, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Abstract:
The lysine acetyltransferase 6A (KAT6A, MOZ, MYST3) is a member of the MYST family of protein acetyltransferases, which are essential for different biological processes such as craniofacial, embryonic, stem cell development, and hematopoiesis. KAT6A is an oncogene in human acute myeloid leukemia (AML), and KAT6A overexpression in AML is associated with metastases and poor prognoses. Furthermore, KAT6A mutations play an important role in cancer formation and progression and result in therapeutic resistance in both hematopoietic malignancies and solid tumors. In this review, we discuss the structural and biological functions of KAT6A and summarize the influence of KAT6A in the development of various tumors. In addition, the recent KAT6A/B inhibitors, their anticancer activities, challenges, and perspective of developing KAT6A/B inhibitors as anticancer drug candidates were introduced.
Insights
Lysine acetyltransferase 6A (KAT6A) is crucial for development and acts as an oncogene in acute myeloid leukemia (AML). This review covers KAT6A functions, its role in cancer, and emerging KAT6A/B inhibitors for cancer therapy.
Area of Science:
- Molecular Biology
- Oncology
- Biochemistry
Background:
- Lysine acetyltransferase 6A (KAT6A) is a MYST family member vital for development and hematopoiesis.
- KAT6A functions as an oncogene in acute myeloid leukemia (AML), linked to poor prognosis and metastasis.
- KAT6A mutations contribute to cancer progression and therapeutic resistance in various cancers.
Purpose of the Study:
- To review the structural and biological functions of KAT6A.
- To summarize KAT6A's role in the development of diverse tumors.
- To introduce recent KAT6A/B inhibitors, their anticancer activities, and future therapeutic potential.
Main Methods:
- Literature review of structural and biological functions of KAT6A.
- Summary of KAT6A's influence on tumor development.
- Overview of recent research on KAT6A/B inhibitors and their therapeutic applications.
Main Results:
- KAT6A is essential for normal development but acts as an oncogene in AML.
- KAT6A overexpression and mutations are implicated in cancer progression and drug resistance.
- Emerging KAT6A/B inhibitors show promise as anticancer drug candidates.
Conclusions:
- KAT6A plays a dual role in development and oncogenesis.
- Targeting KAT6A presents a potential therapeutic strategy for various cancers.
- Further development of KAT6A/B inhibitors is warranted for clinical application.
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