Mode of action | Target | Compound name | Types of cancer | Reference |
---|---|---|---|---|
Enzymatic inhibition | DOT1L | EPZ-5676 | MLL-rearranged leukemia | |
EZH2 | EPZ6438, GSK126, CPI-1205 | Lymphoma, malignant rhabdoid tumor | ||
p300 | C646, A-485 | hematological malignancies and androgen receptor-positive prostate cancer | [88] | |
HDACs | Vorinostat, romidepsin | CTCL | ||
CARM1 | EZM2302 | Multiple myeloma | [91] | |
PPI disruption | Menin-MLL | MI-503, MI-463, M-525 | MLL-rearranged leukemia | |
WDR5-MLL | OICR-9429 | C/EBPα N-terminal leukemia | [84] | |
LEDGF-MLL | CP65 | MLL-rearranged leukemia | [92] | |
Competitive binding | BET family of BRD proteins | JQ1, I-BET, I-BET151 | NUT midline carcinoma, MLL-rearranged leukemia | |
Protein degradation | BRD4 | dBET1, dBET6, ARV-825, ARV-771, BETd-246 | AML, T-ALL, Burkitt’s lymphoma, castration-resistant prostate cancer, TNBC |