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Table 1 Epigenetic-related synthetic lethal relationships and mechanisms in different

From: Epigenetic synthetic lethality approaches in cancer therapy

Gene Inhibitor Cancer type Mechanism References
Epigenetic alterations with epigenetic inhibitors
 ARID1A EZH2 i OCCC Epigenetic antagonism with PRC2 [11]
SMARCB1 EZH2 i MRTs and ATRT Restores expression of p16INK4a [17, 20]
SMARCB1 HDAC i MRTs and ATRT Mimics HAT activity [16]
CREBBP p300 i Lung Cancer
Hematopoietic cancer
Reduces acetylation of MYC promoter [23]
MLL DOT1L i Leukemia (MLL) Reduces H3K79 methylation levels, interfering expression of MLL-fusion target gene inhibit LAMP5 and promote autophagy [34,35,36,37,38]
Epigenetic alterations with non-epigenetic inhibitors
SETD2 WEE1 i Kidney cancer mast cell leukemia Starves the cells of dNTPs [40, 46]
SETD2 PI3Kβ-AKT i Kidney cancer Inhibition of the PI3Kβ-AKT axis [50]
KMT2C PARP i Bladder cancer
Colon cancer
NSCLC HNSCC
Blocks HR-mediated DNA repair [58]
Non-epigenetic alterations with epigenetic inhibitors
TP53 EZH2 i Breast cancer
Prostate cancer
Blocks the binding of EZH2 and p53 [64]