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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]