期刊
JOURNAL OF HEMATOLOGY & ONCOLOGY
卷 14, 期 1, 页码 -出版社
BMC
DOI: 10.1186/s13045-021-01041-1
关键词
KDM5A; Cancer; Jumonji C domain; Histone methylation; Drug resistance; Targeted therapy
资金
- Natural Science Foundation of Zhejiang Province [LZ18C190001]
- Hong Kong Baptist University [FRG2/17-18/003]
- Health and Medical Research Fund [HMRF/14150561]
- National Natural Science Foundation of China [22077109, 21775131]
- Hong Kong Baptist university Century Club Sponsorship Scheme 2020
- Interdisciplinary Research Matching Scheme [RC-IRMS/15-16/03]
- Science and Technology Development Fund, Macao SAR [0072/2020/A2]
- University of Macau [MYRG2019-00002-ICMS]
Histone methylation is crucial for chromatin function, affecting genome integrity, transcriptional regulation, and epigenetic inheritance. KDM5A, a key demethylase, plays a significant role in various human diseases, particularly cancers. Research on KDM5A inhibitors for cancer therapy shows promise but also presents challenges in the field.
Histone methylation is a key posttranslational modification of chromatin, and its dysregulation affects a wide array of nuclear activities including the maintenance of genome integrity, transcriptional regulation, and epigenetic inheritance. Variations in the pattern of histone methylation influence both physiological and pathological events. Lysine-specific demethylase 5A (KDM5A, also known as JARID1A or RBP2) is a KDM5 Jumonji histone demethylase subfamily member that erases di- and tri-methyl groups from lysine 4 of histone H3. Emerging studies indicate that KDM5A is responsible for driving multiple human diseases, particularly cancers. In this review, we summarize the roles of KDM5A in human cancers, survey the field of KDM5A inhibitors including their anticancer activity and modes of action, and the current challenges and potential opportunities of this field.
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