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Hypoxia-inducible factors

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Hypoxia-inducible factors (HIFs) are transcription factors that regulate the cellular biological response to hypoxic stress. They regulate the expression of genes that contain hypoxia response elements (HREs), which produce proteins that coordinate to regulate biological processes including angiogenesis, proliferation, migration, and immune evasion [2]. HIFs are implicated in tumour growth and progression via their interactions with oncoproteins and tumour suppressors [1]. HIF inhibitors are in clinical development as cancer therapeutics.

Targets

3148
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HIF-2α (endothelial PAS domain protein 1) Show summary »


Target Id 3148
Nomenclature endothelial PAS domain protein 1
Common abbreviation HIF-2α
Previous and unofficial names HIF2A | PASD2
Genes EPAS1 (Hs), Epas1 (Mm), Epas1 (Rn)
Ensembl ID ENSG00000116016 (Hs), ENSMUSG00000024140 (Mm), ENSRNOG00000021318 (Rn)
UniProtKB AC Q99814 (Hs), P97481 (Mm), Q9JHS1 (Rn)
Inhibitors
PT2385 (Binding) pKd 7.3 [3]
belzutifan (Binding) pIC50 8.1 [4]

References

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How to cite this family page

Database page citation:

Hypoxia-inducible factors. Accessed on 25/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=1043.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Buneman OP, Faccenda E, Harding SD, Spedding M, Cidlowski JA, Fabbro D, Davenport AP, Striessnig J, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Introduction and Other Protein Targets. Br J Pharmacol. 180 Suppl 2:S1-22.