期刊
PHARMACOLOGICAL RESEARCH
卷 173, 期 -, 页码 -出版社
ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD
DOI: 10.1016/j.phrs.2021.105888
关键词
Anticancer; Epigenetic; Histone methyltransferase; NSD1; SET domain
资金
- Macao Science and Technology Development Fund (Macau Centre for Research and Development in Chinese Medicine) [007/2020/ALC]
- Research Fund of University of Macau [CPG2021-00022-ICMS]
- China Postdoctoral Science Foundation [2017M622811]
- Natural Science Foundation of Guangdong Province, China [2018A030310226, 2020A1515010922]
- Educational Commission of Guangdong Province, China [2017KQNCX084]
- Traditional Chinese Medicine Bureau of Guangdong Province, China [20201183]
- Southwest Medical University [41/00040179]
NSD1 is a bifunctional protein involved in gene regulation, DNA repair, and various biological processes, with implications in different types of cancers. Research on NSD1 lays the foundation for tumor therapy and inhibitor development.
Nuclear receptor binding SET Domain Protein 1 (NSD1) is a bifunctional transcriptional regulatory protein that encodes histone methyltransferase. Mono- and di-methylation of H3K36 by NSD1 is mainly primarily involved in the regulation of gene expression, DNA repair, alternative splicing, and other important biological processes. Many types of cancers, including acute myelogenous leukemia (AML), liver cancer, lung cancer, endometrial carcinoma, colorectal cancer, and pancreatic cancer, are associated with NSD1 fusion, missense mutation, nonsense mutation, silent mutation, deletion, and insertion of frameshift, and deletion in a frame. Therefore, targeting NSD1 may be a potential strategy for tumor therapy. An in-depth study of the structure and biological activities of NSD1 sets the groundwork for improving tumor therapy and creating NSD1 inhibitors. This article emphasizes the role of NSD1 in tumorigenesis and the development of NSD1 targeted small-molecule inhibitors.
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