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.

KDM5B（赖氨酸特异性脱甲基酶5B）从H3K4me2 / 3清除甲基，这对染色质结构具有广泛的调节作用，并抑制基因的转录功能。KDM5B作为癌基因起作用，并与人类癌症密切相关。自从有效的KDM5B抑制剂CPI-455出现以来，靶向KDM5B一直是治愈癌症的有希望的方向。在这一领域，大多数报道的KDM5B抑制剂是Fe（Ⅱ）螯合剂，它们在活性口袋中也与辅因子2-OG竞争。此外，通过高通量筛选或生化筛选已鉴定出一些KDM5B抑制剂。在这篇综述文章中，我们总结了KDM5B的开拓性进展，以提供全面的实现，包括晶体结构，转录调控功能，与癌症相关的功能，抑制剂的开发和SAR研究。我们希望提供KDM5B的全面概述以及KDM5B抑制剂的开发。