HIF

In silico and in vitro human metabolism of IOX2, a performance-enhancing doping agent

21 views | Jan 10 2024

The study successfully identified thirteen metabolites of IOX2 in human hepatocytes, with hydroxyquinolinyl-IOX2 emerging as a major biomarker, emphasizing the critical role of glucuronide hydrolysis for enhanced detectability in urine, offering valuable insights for anti-doping testing. [Read the Full Post]

NHWD-870 protects the kidney from ischemia/reperfusion injury by upregulating the PI3K/AKT signaling pathway (experimental study)

49 views | Dec 23 2023

NHWD-870 exhibits substantial nephroprotective effects by attenuating renal damage through its anti-apoptotic, anti-inflammatory, and antioxidant properties, indicating potential therapeutic promise in managing renal ischemia-reperfusion injury. [Read the Full Post]

Daprodustat: A potential game-changer in renal anemia therapy-A perspective

29 views | Dec 04 2023

As of my last update in September 2021, I cannot confirm the recent FDA approval of daprodustat (DPD) for anemia due to chronic kidney disease in dialysis patients or its potential applications in non-dialysis patients and those with coexisting renal anemia and heart failure; for the latest information, please refer to official sources. [Read the Full Post]

Staphylococcus aureus Infection Initiates Hypoxia-Mediated Transforming Growth Factor-β1 Upregulation to Trigger Osteomyelitis

61 views | Nov 09 2023

This study reveals a novel signaling cascade involving hypoxia/HIF-1α/TGF-β1 in the pathogenesis of Staphylococcus aureus-induced osteomyelitis, highlighting its potential as a therapeutic target for the condition. [Read the Full Post]

Inhibiting HIF-1 signaling alleviates HTRA1-induced RPE senescence in retinal degeneration

28 views | Oct 12 2023

Elevated levels of HTRA1 in age-related macular degeneration (AMD) contribute to retinal pigment epithelium (RPE) senescence by damaging mitochondrial function and activating HIF-1 signaling, suggesting the inhibition of HIF-1 signaling as a potential therapeutic strategy for AMD. [Read the Full Post]

Safety of HIF prolyl hydroxylase inhibitors for anemia in dialysis patients: a systematic review and network meta-analysis

36 views | Sep 18 2023

The systematic review and network meta-analysis found that hypoxia-inducible factor prolyl hydroxylase inhibitors (HIF-PHIs) did not significantly differ from erythropoiesis-stimulating agents (ESAs) in terms of overall adverse events and serious adverse events, but differences were observed in gastrointestinal disorder, hypertension, vascular-access complications, and hemoglobin response. [Read the Full Post]

Evaluation of Drug-Drug Interaction Potential of Enarodustat (JTZ-951) Using a Cytochrome P450 Probe Cocktail

66 views | Sep 17 2023

Enarodustat, administered at doses of 25 mg and 50 mg, showed minimal to no significant drug interactions with cytochrome P450 enzymes 1A2, 2C9, 2C19, 2D6, and 3A4 in a phase 1 multiple-ascending-dose study, with changes in geometric mean ratios generally being less than 2-fold. [Read the Full Post]

Two is company, is three a crowd? Triplet therapy, novel molecular targets, and updates on the management of advanced renal cell carcinoma

68 views | Sep 06 2023

Recent advances in the management of advanced renal cell carcinoma include the favorability of nivolumab plus cabozantinib in combination therapy, promising results from triplet therapy and HIF-2α inhibitors, investigation of metabolic pathway inhibitors and biomarkers, and the ongoing evaluation of cytoreductive nephrectomy in the context of combination therapy. [Read the Full Post]

VH298-loaded extracellular vesicles released from gelatin methacryloyl hydrogel facilitate diabetic wound healing by HIF-1α-mediated enhancement of angiogenesis

61 views | Aug 03 2023

This study demonstrates the potential of VH298-loaded extracellular vesicles (EVs) and GelMA hydrogel as a promising therapeutic strategy for diabetic wound treatment, promoting angiogenesis and enhancing wound healing. [Read the Full Post]

Metabolic study of hypoxia-inducible factor stabilizers BAY 87-2243, MK-8617, and PT-2385 in equine liver microsomes for doping control

49 views | Aug 03 2023

This study identified multiple metabolites, including hydroxylated and glucuronic acid conjugated forms, for the hypoxia-inducible factor-prolyl hydroxylase inhibitor compounds BAY 87-2243, MK-8617, and PT-2385 in equine liver microsomes, shedding light on their metabolic pathways and potential misuse as performance enhancers. [Read the Full Post]