Table 2.
A summary of small molecule inhibitors targeting 20S core proteasome and immunoproteasome.
| Targets | Inhibitors | Chemical nature | Mechanism of action | Developer | Dev. stage |
|---|---|---|---|---|---|
| 20S Core | Bortezomib (PS341) | Boronate | β5 > β1 | Millennium | FDA approved |
| MLN-9708 | Boronate | β5 > β1 | Millennium | Phase I – II | |
| Delanzomib (CEP-18770) | Boronate | β5 > β1 | Cephalon | Phase I – II | |
| Carfizomib (PR-171) | Epoxyketone | β5, β5i | ONXY | FDA approved | |
| Oprozomib (ONX-0912) | Epoxyketone | β5, β5i | ONXY | Phase I – II | |
| Marizomib (NPI-0052) | β-lactone | β5 > β2 > β1 | Nereus | Phase I | |
| Immunoproteasome | ONX-0914 (PR-957) | Boronate | β5i | ONXY | Pre-clinical |
| PR-924 | Boronate | β5i | |||
| IPSI-001 | Aldehyde | β5i, β1i |