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Table 2 HIF targeted agents in cancer therapy

From: Hypoxia-inducible factors: master regulators of hypoxic tumor immune escape

Agents Model Regulatory mechanisms Refs.
17-allyl-amino-geldanamycin Human glioma cell lines Geldanamycin decreases cancer cell migration via HIF1A degradation [169]
PX-478 Esophageal squamous cancer cells HIF1A inhibitor PX-478 promotes apoptosis and inhibits G2/M transition contributing to tumor cell proliferation [170]
PX-12 HT-29 colon carcinoma cell line Thioredoxin-1 inhibitor decreases the tumor vascular permeability by downregulating HIF1A protein levels and VEGF expression [41]
PT2385 Human ccRCC tumor cells HIF2A inhibitor PT2385 hinders cancer metastases by dissociating HIF2A complexes [172]
PT2399 786-O cells
Human ccRCC tumor cells
HIF2A small molecule inhibitor PT2399 causes tumor regression [173]
AFP464 Human cancer cells lines Aminoflavone inhibits HIF1 and HIF2 transcriptional protein accumulation for anti-cancer activity [174]
Acriflavine HEK293 cells
Human P493 cells
Acriflavine inhibits the HIF1 dimerization and has inhibitory effects on tumors growth [175]
Chetomin HCT116 cells Epidithiodiketopiperazines could inhibit the HIF1A-p300 binding via zinc ion ejection [176]