Table 2.
Molecular targeting of HIF signaling
| Inhibitory mechanism | Molecular targets | Targeting agents |
|---|---|---|
| mRNA/protein expression | PI3K | Wortmannin, LY94002, GDC-0941, PI-103 |
| mTOR | Rapamycin, PP242, Glyceollins | |
| Topoisomerase 1 | Topotecan, PEG-SN38 | |
| HIF-1α mRNA | EZN-2968 | |
| Microtubules | 2ME2, ENMD-1198 | |
| Hsp90 | Geldanamycin and analogs | |
| HDAC | Vorinostat | |
| Thioredoxin-1 | PX-12, pleurotin | |
| IRP1/IRE interaction | HIF-2α translational inhibitors | |
| HIF-α/HIF-1β dimerization | HIF-1α/2α PAS-B domain | Acriflavine |
| HIF-2α PAS-B domain | PT2385 | |
| DNA binding | HRE | Echinomycin, Polyamides |
| Transcriptional activity | p300 recruitment | Chetomin, Bortezomib |
| FIH-1 interaction and p300 recruitment | Amphotericin B | |
| Hsp70 | Triptolide | |
| Thioredoxin-1 | AJM290, AW464 |
Adapted from Caroline Wigerup, et al., 2016 [192].