1. Targeting histone demethylase KDM5B for cancer treatment.
- Author
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Fu, Yun-Dong, Huang, Ming-Jie, Guo, Jia-Wen, You, Ya-Zhen, Liu, Hong-Min, Huang, Li-Hua, and Yu, Bin
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DRUG resistance in cancer cells , *CANCER treatment , *BIOMARKERS , *METHYL groups , *DEMETHYLASE - Abstract
KDM5B (Lysine-Specific Demethylase 5B) erases the methyl group from H3K4me2/3, which performs wide regulatory effects on chromatin structure, and represses the transcriptional function of genes. KDM5B functions as an oncogene and associates with human cancers closely. Targeting KDM5B has been a promising direction for curing cancer since the emergence of potent KDM5B inhibitor CPI-455. In this area, most reported KDM5B inhibitors are Fe (Ⅱ) chelators, which also compete with the cofactor 2-OG in the active pockets. Besides, Some KDM5B inhibitors have been identified through high throughput screening or biochemical screening. In this reviewing article, we summarized the pioneering progress in KDM5B to provide a comprehensive realization, including crystal structure, transcriptional regulation function, cancer-related functions, development of inhibitors, and SAR studies. We hope to provide a comprehensive overview of KDM5B and the development of KDM5B inhibitors. Image 1 • KDM5B was overexpressed in many cancers and performd an efficient transcriptional regulation function. • KDM5B was found to be an oncogene and biomarker of many cancers. • KDM5B was associated with cancer immunotherapy and drug resistance. • The SAR studies and developmental strategies of diverse KDM5B inhibitors were discussed. [ABSTRACT FROM AUTHOR]
- Published
- 2020
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