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. 2015 Jan;16(1):32–43. doi: 10.1631/jzus.B1400221

Table 2.

Inhibitors of HIF-1 pathway

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