Background
Classification and function of HMTs
HMTs and its classification
The function of HMTs
The biological characteristics of HMTs
KMTs and tumor biological characteristics
PRMTs and tumor biological characteristics
HMTs and cancer drug resistance
KMTs and cancer drug resistance
H3K27 KMTs and drug resistance
H3K9 KMTs and drug resistance
Other KMTs and drug resistance
PRMTs and cancer drug resistance
PRMT1 and drug resistance
PRMT5 and drug resistance
Other PRMTs and drug resistance
Regulating HMTs on drug resistance in tumors
KMT inhibitors reverse cancer drug resistance
Targeting H3K27 KMTs reverse drug resistance
Targeting H3K9 KMTs reverse drug resistance
Targeting other KMTs reverse drug resistance
PRMT inhibitors reverse cancer drug resistance
Enzyme | Cancer type | Drug | Inhibitor | Mechanism (Reference) |
---|---|---|---|---|
EZH2 | Clear cell renal cell carcinoma | Sunitinib | EPZ011989 | Reduced overall phosphorylation of kinases and increased activation of tumor suppressors [90]. |
Ovarian cancer | Cisplatin | GSK126 | ||
SCLC | Etoposide | GSK126 | Reduced H3K27me3 in CDKN1C promoter, leading to increased CDKN1C expression [93]. | |
Melanoma | Immune checkpoint inhibitors | GSK503 | Decreased H3K27me3 leads to up-regulation of antigen and down-regulation of PD-L1 [94]. | |
G9a | NSCLC | EGFR-TKI | UNC0638 | Regulation of PTEN / AKT pathway is inhibited [68]. |
HNSCC | Cisplatin | UNC0638 | H3K9me1 reduction in GCLC promoter causes an increase in Glutathione expression [65]. | |
GBM | Temozolomide | BIX-01294 | Unknown [95]. | |
Cervical cancer | Gemcitabine | Hydralazine | ||
Hepatocellular Carcinoma | TRAIL | BIX-01294 | Downregulate Survivin [97]. | |
SETD2 | Acute leukemia | Cytarabine, Etoposide | JIB-04 | |
DOT1L | Breast cancer | Antiestrogen | EPZ004777 | Blocked ERα expression [102]. |
MLL1 | Pancreatic cancer | PD-L1 inhibitor | Verticillin A | Reduced H3K4me3 in the CD274 promoter and PD-L1 expression [103]. |
PRMT5 | Breast cancer | CDK4/6 inhibitor (palbociclib) | GSK3326595 | Reduced MDM4 expression leads to p53 activation and the inhibition of CDK2 [104]. |
GBM | mTOR inhibitors | EPZ015666 | Inhibited SDMA methylation in hnRNP A1 and IRES-mediated activation of related proteins [84]. |