Hypoxia-inducible factors (HIF-1 and HIF-2) are essential mediators for the adaptive transcriptional response of cells and tissues to low-oxygen conditions. Under hypoxia or when cells are treated with various nonhypoxic stimuli, the active HIF-α subunits are mainly regulated through increased protein stabilization. For HIF-1α, it is clear that further transcriptional, translational, and posttr...

Hypoxia-inducible factor-1 (HIF-1) is the central mediator of cellular responses to low oxygen and vital to many aspects of cancer biology. In a search for HIF-1 inhibitors, we identified celastrol as an inhibitor of HIF-1 activation from Tripterygium wilfordii. In the present study, we demonstrated the effect of celastrol on HIF-1 activation. Celastrol showed a potent inhibitory activity again...

The transcription factor HIF-1a is essential for cells to rapidly adapt to low oxygen levels (hypoxia). HIF-1a is frequently deregulated in cancer and correlates with poor patient prognosis. Here, we demonstrate that the deubiquitinase Cezanne regulates HIF-1a homeostasis. Loss of Cezanne decreases HIF-1a target gene expression due to a reduction in HIF-1a protein levels. Surprisingly, although...

Accurate in vivo predictions of intestinal absorption low solubility drugs require knowing their physiologically relevant dissolution media. Aspirated human fluids (HIF) are the gold standard, followed by simulated HIF fasted and fed state (FaSSIF/FeSSIF). However, current characterization data vary, there is also some controversy regarding accuracy FaSSIF FeSSIF for predicting drug HIF. This s...

Abstract Background and Aims Anemia is common among patients with chronic kidney disease (CKD) reported to be associated increased cardiovascular all-cause mortality, as well reduced quality of life. The incidence anemia increases function declines affects approximately 32% Japanese stage 3–5 CKD [1]. Hypoxia-inducible factor prolyl hydroxylase inhibitors (HIF-PHIs) have been approved in the Ja...

Cancer cells adapt to hypoxia by the stabilization of hypoxia inducible factor (HIF)-α isoforms that increase the transcription of several genes. Among the genes regulated by HIF are enzymes that play a role in invasion, metastasis and metabolism. We engineered triple (estrogen receptor/progesterone receptor/HER2/neu) negative, invasive MDA-MB-231 and SUM149 human breast cancer cells to silence...

BACKGROUND Hypoxia-inducible factor 1 (HIF)-1alpha is a transcription factor that functions as master regulator of mammalian oxygen homeostasis. In addition, recent studies identified a role for HIF-1alpha as transcriptional regulator during inflammation or infection. Based on studies showing that respiratory syncytial virus (RSV) is among the most potent biological stimuli to induce an inflamm...

Abstract Background Tumor protein D52 (TPD52) reportedly plays an important role in the proliferation and metastasis of various cancer cells, including oral squamous cell carcinoma (OSCC) is expressed strongly at center tumor, where microenvironment hypoxic. Thus, present study investigated roles TPD52 survival death OSCC cells under hypoxia, relationship with hypoxia-inducible factor (HIF). We...

With great interest, I read the impressive new findings by Hanudel et al. recently published in Kidney International showing that erythroferrone-mediated suppression of hepcidin is not essential for beneficial effects vadadustat, as hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), on anemia chronic kidney disease.1 In discussion section, authors meticulously listed several alter...

Hypoxia-inducible factor (HIF)-1α and HIF-2α are the main regulators of cellular responses to hypoxia. Post-translational modifications of HIF-1α and 2α are necessary to modulate their functions. The methylation of non-histone proteins by Set7, an SET domain-containing lysine methyltransferase, is a novel regulatory mechanism to control cell protein function in response to various cellular stre...