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TRIOL attenuates intracerebral hemorrhage injury by bidirectionally modulating microglia- and neuron-mediated hematoma clearance.
Redox Biol
December 2024
Department of Biochemistry and Molecular Biology, Zhongshan School of Medicine, Sun Yat-Sen University, Guangzhou, 510080, China. Electronic address:
Intracerebral hemorrhage (ICH) represents the most severe subtype of stroke, and the lack of effective clinical pharmacotherapies poses a substantial threat to human health. Hematoma plays a crucial role in determining the prognosis of ICH patients by causing primary mechanical extrusion, followed by secondary brain injuries, such as cerebral edema, iron-mediated oxidative stress, and inflammation resulting from its degradation products. 5α-androst-3β,5α,6β-triol (TRIOL) is a neuroprotective steroid currently undergoing phase II clinical trial for acute ischemic stroke with anti-oxidative and anti-inflammatory properties.
View Article and Find Full Text PDFHighly Selective Novel Heme Oxygenase-1 Hits Found by DNA-Encoded Library Machine Learning beyond the DEL Chemical Space.
ACS Med Chem Lett
September 2024
WuXi AppTec, 22 Strathmore Road, Natick, Massachusetts 01760, United States.
Article Synopsis
- DNA-encoded library (DEL) technology combined with machine learning (ML) helps in discovering new drug inhibitors effectively and cost-efficiently.
- The study focuses on heme oxygenase-1 (HO-1), an enzyme linked to serious diseases, and reports the discovery of five new series of potential inhibitors using a DEL-ML approach.
- Notably, 37% of the new molecules showed strong binding affinity to HO-1, with some demonstrating over 100-fold selectivity for HO-1 compared to related enzymes, showcasing their structural novelty and potential for further research.
Association of total bilirubin and prognosis in disorders of consciousness.
Sci Rep
August 2024
Department of Rehabilitation Medicine, The Second Hospital of Shandong University, 247# Beiyuan Street, Jinan, 250033, Shandong, China.
Accurate prediction of the recovery of Disorders of Consciousness (DoC) is of paramount significance for clinicians and families. Serum total bilirubin (TBIL) formed by activation of heme oxygenase 2, is associated with incidence and prognosis of cardiovascular and cerebrovascular diseases. However, studies that based TBIL and DoC are limited.
View Article and Find Full Text PDFTargeting Heme Oxygenase 2 (HO2) with TiNIR, a Theragnostic Approach for Managing Metastatic Non-Small Cell Lung Cancer.
Biomater Res
April 2024
Department of Biomedical Science, Sunchon National University, Suncheon 57922, Republic of Korea.
Article Synopsis
- Despite improvements in cancer treatments, metastasis still poses a significant challenge to patient outcomes.
- The research highlights heme oxygenase 2 (HO2) as a potential therapeutic biomarker that can be targeted to combat aggressive cancer subtypes.
- By inhibiting HO2, researchers found reduced cancer cell growth and movement, and demonstrated success in preventing metastasis in mouse models, suggesting that HO2 targeting could improve cancer therapy effectiveness.
'NO-how' enzymatic S-nitrosylation controls insulin pathophysiology.
Trends Endocrinol Metab
February 2024
Redox Biology, Danish Cancer Institute, Strandboulevarden 49, 2100, Copenhagen, Denmark; Department of Biology, Tor Vergata University, Via della Ricerca Scientifica, 00133, Rome, Italy. Electronic address:
Whether S-nitrosylation is the result of an unselective chemical process or enzymatically driven has been debated for years. A recent study by Zhou et al. identifies and characterizes the first S-nitroso-CoA (SNO-CoA)-assisted nitrosylase (SCAN) that catalyzes protein S-nitrosylation in mammals, including insulin receptor (INSR)/insulin receptor substrate 1 (IRS1), with implications for human metabolism.
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