Table 1.
Reported E1, E3, proteasome, deubiquitinase enzyme and aminopeptidase modulators in clinical trials.
| Modulators | Target | Clinical Stage |
|---|---|---|
| E1 enzyme modulators | ||
| MLN7243 | Ubiquitin-Activating Enzyme (Uba1) | Phase 1 completed |
| E3 enzyme modulators | ||
| APG-115 | MDM2-p53 | Phase 1 recruiting |
| ALRN 6924 | MDM2\MDMX | Phase 1 |
| CC-122 | Cereblon (CRBN) | Phase 1\2 |
| Indisulam | Cullin-4A-DCAF15 | Phase 2 completed |
| CQS | ||
| Tasisulam | Phase 3 terminated | |
| Proteasome Inhibitors alone or in combination with other drugs | ||
| Bortezomib + Idarubicin + Cytarabine | Proteasome B5 protease | Phase 1 |
| Bortezomib + Daunorubicin+ Cytarabine | ||
| Bortezomib + Decytabine | Phase 2 | |
| Bortezomib + SAHA | Phase 2 suspended | |
| Carlfizomib | Phase 1 | |
| Deubiquitinase inhibitors modulators | ||
| VLX1570 | Ubiquitin Specific Peptidase 14,Ubiquitin C-terminal hydrolase 37 | Phase 1\2 suspended |
| Aminopeptidase inhibitors in combination with other drugs | ||
| Tosedostat + Decytabine | Leukotriene A4LTA4, Aminopeptidase N, Leucine aminopeptidase PuSA | Phase 2 |
| Tosedostat + Cytarabine | ||
| Immunomodulatory (IMiDs) drugs | ||
| CC-122 | Ikaros family zinc finger protein 1 IKZF1 and IKZF3 | Phase 1\2 |