2. Academic Validation
  3. Recent advances in targeting histone H3 lysine 36 methyltransferases for cancer therapy

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

  • Eur J Med Chem. 2024 Aug 5:274:116532. doi: 10.1016/j.ejmech.2024.116532.
Sai Ma 1,  Guanlu Long 1,  Zheng Jiang 1,  Yan Zhang 1,  Liangkui Sun 1,  Yun Pan 2,  Qidong You 3,  Xiaoke Guo 4
Affiliations

Affiliations

  • 1 Jiangsu Key Laboratory of Drug Design and Optimization and State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, China.
  • 2 Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
  • 3 Jiangsu Key Laboratory of Drug Design and Optimization and State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China. Electronic address: [email protected].
  • 4 Jiangsu Key Laboratory of Drug Design and Optimization and State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China. Electronic address: [email protected].
PMID: 38805937 DOI: 10.1016/j.ejmech.2024.116532
Abstract

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.

Keywords

Cancers; H3K36; HKMTs; Inhibitors.

Figures