Recent advances in targeting histone H3 lysine 36 methyltransferases for cancer therapy

被引：4
|
作者：
Ma, Sai [1 ,2 ]
Long, Guanlu [1 ,2 ]
Jiang, Zheng [1 ,2 ]
Zhang, Yan [1 ,2 ]
Sun, Liangkui [1 ,2 ]
Pan, Yun [3 ]
You, Qidong [1 ,2 ,3 ,4 ]
Guo, Xiaoke [1 ,2 ,3 ,4 ]
机构：
[1] China Pharmaceut Univ, Jiangsu Key Lab Drug Design & Optimizat, Nanjing 210009, Peoples R China
[2] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Peoples R China
[3] China Pharmaceut Univ, Sch Pharm, Dept Med Chem, Nanjing 210009, Peoples R China
[4] China Pharmaceut Univ, Sch Pharm, Jiang Su Key Lab Drug Design & Optimizat, Nanjing 210009, Peoples R China
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2024年 / 274卷
基金：
中国国家自然科学基金;
关键词：
HKMTs; Cancers; Inhibitors; CELL-PROLIFERATION; DOWN-REGULATION; NSD FAMILY; SETD2; GENE; PROTEIN; METHYLATION; METASTASIS; DISCOVERY; CARCINOMA;
D O I：
10.1016/j.ejmech.2024.116532
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Histone H3 lysine 36 (H3K36) methylation is a typical epigenetic histone modification that is involved in various biological processes such as DNA transcription, repair and recombination in vivo. Mutations, translocations, and aberrant gene expression associated with H3K36 methyltransferases have been implicated in different malignancies such as acute myeloid leukemia, lung cancer, multiple myeloma, and others. Herein, we provided a comprehensive overview of the latest advances in small molecule inhibitors targeting H3K36 methyltransferases. We analyzed the structures and biological functions of the H3K36 methyltransferases family members. Additionally, we discussed the potential directions for future development of inhibitors targeting H3K36 methyltransferases.
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页数：18
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