Table 1 Reported studies evaluating BET-PROTACs
From: Proteolysis targeting chimeras (PROTACs) in cancer therapy
Transcription factor | Ligand for E3 ligases | Cancer type | BET Inhibitor | PROTAC | Reference |
|---|---|---|---|---|---|
BRD4 | Von Hippel-Lindau (VHL) E3 ligase, E3 ubiquitin ligase CRBN | Osteosarcoma, leukemia | JQ1 | BETd-260 | [36] |
BRD4 | E3 ubiquitin ligase CRBN | Leukemia, Burkitts Lymphoma | Oxazepines, JQ1, OTX | QCA570, ARV-825 | |
BRD1, BRD2 and BRD4 | E3 ubiquitin ligase CRBN | Burkitt’s lymphoma | JQ1, OTX | ARV-825 | [34] |
BRD4 over BRD2 and BRD3 | Von Hippel-Lindau (VHL) E3 ligase | Cervical carcinoma | JQ1 | MZ1 | [33] |
BRD4 | Von Hippel-Lindau (VHL) E3 ligase | Triple negative Breast Cancer and JQ1 resistant cells | JQ1 | MZ1 | [38] |
OTX | ARV-825 | ||||
BRD2, BRD3 and BRD4 | E3 ubiquitin ligase CRBN | Leukemia | JQ1 | dBET1 | [31] |
BRD2, BRD3 and BRD4 | E3 ubiquitin ligase CRBN | Triple negative Breast Cancer | BETi-211 | BETd-246 | [39] |
Pan BET degrader | Von Hippel-Lindau (VHL) E3 ligase | Prostate cancer | BETinhibitor | ARV-771 | [40] |
Bromodomain containing proteins: BRD9 | E3 ubiquitin ligase CRBN | AML | BRD9 inhibitor | dBRD9 | [41] |
Bromodomain containing proteins: BRD7/BRD9 | Von Hippel-Lindau (VHL) E3 ligase | Leukemia | BRD9/BRD7 inhibitor | VZ185 | [42] |