Table 1 Drugs that influence ubiquitin-proteasome activity
Drug class | Action and mechanism |
|---|---|
Chemotherapeutic agents | |
Aclarubicin | Inhibits the chymotrypsin-like proteolytic activity of the proteasome |
All-trans retinoic acid | May accelerate PML fusion protein degradation through the proteasome |
Arsenic trioxide | Inhibits ubiquitination and degradation of IκB through effects on the IκB kinase |
Camptothecin | Stimulate ubiquitination and degradation of topoisomerase 1 |
Geldanamycin | Inhibits HSP90 ATPase, stimulating proteasomal degradation of client proteins |
PS-341/LDP-341/MLN-341 | Inhibits the chymotrypsin-like activity of the proteasome |
Vinblastine, Vincristine | Inhibit the chymotrypsin-like, trypsin-like- and peptidyl-glutamyl peptide hydrolyzing proteasome activities |
Immunosuppressive agents | |
Cyclosporine A | Uncompetitive inhibitor of the proteasomal chymotrypsin-like activity |
Rapamycin | Inhibits proteasome function by inhibiting the proteasome activator PA28 |
Miscellaneous agents | |
Fulvestrant | Stimulates proteasome-dependent proteolysis of ERα |
Tannic acid | Inhibits the chymotrypsin-like activity of the proteasome |
Lovastatin | Mechanism unknown, but appears structurally similar to the proteasome inhibitor lactacystin |
Anti-retroviral drugs | Inhibit the chymotrypsin-like and trypsin-like proteasome activities |