HIFs (Hypoxia-inducible factors) are transcription factors that react to variations in the amount of oxygen available to cells, more specifically, to reductions in oxygen, or hypoxia. The effects of hypoxia, a condition of low oxygen concentration, on the cell are mediated by the HIF signaling cascade. Oftentimes, hypoxia prevents cells from differentiating. However, hypoxia encourages the growth of blood vessels and is crucial for the development of a vascular system in both cancer tumors and embryos. Additionally, the hypoxia in wounds encourages keratinocyte migration and epithelium repair. HIFs are essential to development in general. HIF-1 gene deletion in mammals causes perinatal death. It has been demonstrated that HIF-1 is essential for chondrocyte survival and enables the cells to adapt to low oxygen environments in the growth plates of bones. Human metabolism is controlled in large part by HIF. A number of medications that function as selective HIF prolyl hydroxylase inhibitors have recently been created.
|Desidustat is an antianaemic drug candidate under investigation for the treatment of anemia of chronic kidney disease.
|IDF-11774 (IDF11774) is a novel, potent, and orally bioavailable HIF-1α (hypoxia-inducible factor 1α) inhibitor with anticancer activity.
|OX4 is a potent inhibitor of PHD2 (IC50 = 1.6 nM).
|PT2399 is a novel, potent, andorally bioavailable small molecule inhibitor of HIF-2 whichbinds to HIF-2α PAS B domain with an IC50 of 6 nM, exhibiting potent antitumor activity in vivo.
|TP0463518 is a novel and potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor.