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Table 2 Examples of inhibitors for chromatin-related proteins

From: Epigenetic modifications of histones in cancer

Mode of action

Target

Compound name

Types of cancer

Reference

Enzymatic inhibition

DOT1L

EPZ-5676

MLL-rearranged leukemia

[85, 86]

EZH2

EPZ6438, GSK126, CPI-1205

Lymphoma, malignant rhabdoid tumor

[9, 77, 87]

p300

C646, A-485

hematological malignancies and androgen receptor-positive prostate cancer

[88]

HDACs

Vorinostat, romidepsin

CTCL

[89, 90]

CARM1

EZM2302

Multiple myeloma

[91]

PPI disruption

Menin-MLL

MI-503, MI-463, M-525

MLL-rearranged leukemia

[82, 83]

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

[93,94,95]

Protein degradation

BRD4

dBET1, dBET6, ARV-825, ARV-771, BETd-246

AML, T-ALL, Burkitt’s lymphoma, castration-resistant prostate cancer, TNBC

[96, 97]