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Targeting histone demethylase KDM5B for cancer treatment.
- Source :
-
European Journal of Medicinal Chemistry . Dec2020, Vol. 208, pN.PAG-N.PAG. 1p. - Publication Year :
- 2020
-
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]
Details
- Language :
- English
- ISSN :
- 02235234
- Volume :
- 208
- Database :
- Academic Search Index
- Journal :
- European Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 147020322
- Full Text :
- https://doi.org/10.1016/j.ejmech.2020.112760