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  • Bidirectional modulation of HIF-2 activity through chemical ligands (2024)

    FAQs

    What does HIF 2 do? ›

    Finally, it was shown that, when endogenous NF-κB is induced by TNFα (tumour necrosis factor α) treatment, HIF-1α levels also change in an NF-κB-dependent manner. HIF-1 and HIF-2 have different physiological roles. HIF-2 regulates erythropoietin production in adult life.

    What is the HIF 2 alpha expression? ›

    HIF-2α is expressed in endothelial cells, the parenchyma and interstitial cells of multiple organs. Although HIF-2α is stabilized at higher O2 pressure compared with HIF-1α in vitro, it was not detected under normoxic conditions in various organs.

    What are the benefits of HIF? ›

    HIF stimulates the body's production of the hormone erythropoietin (EPO), which enables the bone marrow to produce red blood cells.

    What is HIF used for? ›

    Hypoxia-inducible factor (HIF)− 1 is a transcriptional activator dependent on oxygen, which plays an important role in maintaining oxygen homeostasis by regulating the expression of genes associated with adaptation to hypoxia.

    What is the difference between HIF-1 and HIF 2? ›

    Although both isoforms may upregulate the expression of pro-angiogenic vascular endothelial growth factor (VEGF), HIF-1 diminished the expression of interleukin-8 (IL-8) by inhibition of the Nrf2 transcription factor whereas HIF-2 augmented expression of IL-8 in an Nrf2-independent way but via upregulation of SP-1 ...

    What does HIF bind to? ›

    The heterodimeric transactivating complex HIF then binds to the HRE in promoter or enhancer sequences of target genes (Figure 1). The HIF-modifying enzymes were identified as related to egl-9 in Caenorhabditis elegans and termed prolyl hydroxylase domain (PHD) enzymes (PHD1–PHD3).

    What genes does HIF regulate? ›

    HIF-1 modulates the expression of the genes encoding erythropoietin (EPO) and vascular endothelial growth factor (VEGF), and the genes that are involved in glucose transport or glycolysis, e.g., glucose transporter-1 (GLUT1), pyruvate dehydrogenase kinase 1 (PDK1), and lactate dehydrogenase A (LDHA) (Leu et al., 2019).

    What is the difference between HIF-1 and Hif 2? ›

    Although both HIF-1a and HIF-2a are expressed in growth plate chondrocytes, HIF-1a is expressed at similar levels during all stages of chondrocyte differentiation, and its activity is enhanced by hypoxia, whereas HIF-2a levels increase with chondrocyte differentiation, and its function is indepen- dent of oxygen- ...

    What is the role of hif2alpha? ›

    Indeed, HIF-2α has been shown to regulate multiple aspects of angiogenesis, including cell proliferation, migration, maturation of blood vessels, and metastasis. These findings make HIF-2α a critical regulator of physiological and pathological angiogenic phenotype.

    How does HIF increase performance? ›

    The target genes of HIF-1 increase oxygen transport through mechanisms such as erythropoietin-mediated erythropoiesis and vascular endothelial growth factor-induced angiogenesis and improve tissue function during low oxygen availability through increased expression of glucose transporters and glycolytic enzymes, which ...

    What are the effects of HIF? ›

    Activation of HIF induces various effector pathways that mitigate the effects of hypoxia, including metabolic reprogramming and the production of erythropoietin. Drugs that target the HIF pathway to induce erythropoietin production are now approved for the treatment of chronic kidney disease-related anaemia.

    References

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