Table 2.
Mechanism of action | Inhibitor |
Inhibition of HIF-1α mRNA | Aminoflavone, GL331 |
Inhibition of HIF-1α protein synthesis | Topoisomerase inhibitors (such as rapamycin, temsirolimus, and everolimus); cardiac glycosides (such as digoxin and digtoxin), microtubule targeting agents (such as 2-methoxyestradiol, epothilone B, and taxotere), topoisomerase inhibitors (such as camptothecin, topotecan, and NSC 644221), oligonucleotides, AF, PX-478 |
Inhibition of HIF-1α protein stabilization | HSP90 inhibitors (such as 17-AAG, 17-DMAG, and apigenin), HDAC inhibitors (such as FK228 and LAQ824), antioxidants (such as ascorbic acid), oligonucleotides, selenium compound (such as berberine and MSC), PX-12, YC-1 |
Inhibition of HIF-1α:HIF-1β dimerization | Acriflavine |
Inhibitions of HIF-1:DNA binding | Anthracyclines, echinomycin |
Inhibition of HIF-1 transactivity | Bortezomib |
HSP90: heat-shock protein 90; 17-AAG: 17-allylamino-demethoxygeldanamycin; HDAC: histone deacetylase; MSC: methylselenocysteine; 17-DMAG: 17-dimethylaminoethylamino-17-demethoxygeldanamycin