Table 2.
Therapeutic SEs and inhibitors.
SE inhibitor | Molecular target | Function | Tumor type | Ref. |
---|---|---|---|---|
JQ1 | BRD4 | Reducing BRD4 occupancy and MED1 binding, Pol II stalling and elongation impairment | AML | 74,79 |
IBET | CDKs | Regulating RNAPII initiation and elongation | Unascertained | 81 |
THZ1 | CDK7 | Inhibiting phosphorylation of CTD of RNA Pol II and hindering promoter proximal pausing | Neuroblastoma | 65 |
MYCN | Repression of MYCN-dependent transcriptional amplification | Neuroblastoma | 65 |
AML acute myeloid leukemia, BRD4 bromodomain-containing protein 4, CDK cyclin-dependent kinase, CTD carboxyl-terminal domain, Pol II polymerase II.