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Table 2 Examples of inhibitors for chromatin-related proteins

From: Epigenetic modifications of histones in cancer

Mode of actionTargetCompound nameTypes of cancerReference
Enzymatic inhibitionDOT1LEPZ-5676MLL-rearranged leukemia[85, 86]
EZH2EPZ6438, GSK126, CPI-1205Lymphoma, malignant rhabdoid tumor[9, 77, 87]
p300C646, A-485hematological malignancies and androgen receptor-positive prostate cancer[88]
HDACsVorinostat, romidepsinCTCL[89, 90]
CARM1EZM2302Multiple myeloma[91]
PPI disruptionMenin-MLLMI-503, MI-463, M-525MLL-rearranged leukemia[82, 83]
WDR5-MLLOICR-9429C/EBPα N-terminal leukemia[84]
LEDGF-MLLCP65MLL-rearranged leukemia[92]
Competitive bindingBET family of BRD proteinsJQ1, I-BET, I-BET151NUT midline carcinoma, MLL-rearranged leukemia[93,94,95]
Protein degradationBRD4dBET1, dBET6, ARV-825, ARV-771, BETd-246AML, T-ALL, Burkitt’s lymphoma, castration-resistant prostate cancer, TNBC[96, 97]