Mechanisms of HIF-driven immunosuppression in tumour microenvironment

Bandopadhyay, Shinjini; Patranabis, Somi

doi:10.1186/s43046-023-00186-z

Journal of the Egyptian National Cancer Institute

Table 1 HIF-1/2 and downstream target inhibitor drugs and clinical efficacy

From: Mechanisms of HIF-driven immunosuppression in tumour microenvironment

Drug	Target	Mechanism of inhibition	Tumour	Ref.
Acriflavine	HIF-1	Prevents HIF-1α/HIF-1β dimerization	Prostate and colorectal cancer	[91, 95]
Anthracyclines	HIF-1	Inhibits HIF-1 transcriptional activity	Hepatocellular carcinoma, prostate cancer	[92]
Cardenolides	HIF-1	Inhibits HIF-1 transcriptional activity	Breast cancer	[96]
PT2385	HIF-2	Disrupts HIF-2α/ARNT heterodimerization and inhibits HIF-2α target gene expression	Clear cell renal cell carcinoma	[93]
MK-6482	HIF-2		Clear cell renal cell carcinoma	[94]
Benzopyranyl triazole	HIF-1	Increases HIF-1α hydroxylation and subsequent HIF-1α protein degradation	Used in combination with EGFR inhibitor gefitinib in lung and breast cancer	[97]
BIX01294 at low dosage	HIF-1		Hepatocellular carcinoma	[98]
IDF-1174	HIF-1	Increases HIF-1α protein degradation	Hepatocellular carcinoma, colorectal carcinoma	[99]
LBH589			Diffuse large B-cell lymphoma, Hodgkin lymphoma, multiple myeloma, hepatocellular carcinoma, pancreatic cancer and NSCLC	[99]
MPT0G157			Colorectal cancer	[100]
Vorinostat	HIF-1, HIF-2	Decreases HIF-1/2α translation/nuclear localization/stability, increases HIF-1/2 degradation	Hepatocellular carcinoma	[99]
Trastuzumab (Herceptin)	HIF-1 targets	Target oncogenic growth factor signalling pathways regulated by HIF-1	Breast cancer	[24]
Imatinib	HIF-1 targets		Gastric gastrointestinal stromal tumours	[24]
Galunisertib	HIF-1 targets	TGFβRI kinase inhibitor	Breast, colon, lung cancers, and hepatocellular carcinoma	[24]
Lenvatinib	HIF-1 targets	VEGF inhibitor	Hepatocellular carcinoma	[101]
SCH58261	HIF-1/2 targets	A2AR antagonist; inhibits immunosuppressive adenosine in TME	Head and neck squamous cell carcinoma	[102]

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