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. 2023 Feb 17;8:69. doi: 10.1038/s41392-023-01341-7

Table 4.

Histone demethylase inhibitors and siRNA for overcoming drug resistance

Regulatory factor Enzyme Cancer type Mechanism Reference
Arborinine LSD1 Gastric cancer Inhibit the expression of LSD1 and EMT 345
HCI-2509 LSD1 Prostate cancer Inhibit colony-forming ability and reduce the expression of C-MYC to inhibit proliferation 346
GSK2879552 LSD1 Hepatoma Reduce the level of LINC01134 271
NCL1 LSD1 Breast cancer Inhibit LSD1 and cell proliferation and autophagy 347,348
NSC636819 KDM4A Lung, breast, and prostate cancer Increase the expression of DR5 and TRAIL and activate exogenous apoptosis 349
ML324 KDM4B Prostate cancer Inhibit the demethylation activity of KDM4B 298
JIB-04 KDM4A leukemia Increase H3K36me3 level and restore the sensitivity to cytosine arabinoside 350
ZINC33576 KDM5A Breast Cancer Inhibit the demethylation activity of KDM5A to H3K4 and block the cell in G1 phase 352
PBIT KDM5B Non-small cell carcinoma Inhibit lung cancer stem cells like phenotype to regulate cell sensitivity 308
CPI-455 KDM5A APL Promote cell differentiation induced by all-trans retinoic acid 358
GSK-J4 KDM6A; KDM6B Colorectal cancer Inhibit the expression of Notch2 and increase the sensitivity to oxaliplatin 329
KDM2B Hepatoma Reduce the self-renewal ability of stem cells 282
Circ0006168 KDM3C ESCC Positively regulate the expression of KDM3C 290