NADPH-oxidases as potential pharmacological targets for thrombosis and depression comorbidity

Amadio, Patrizia; Sandrini, Leonardo; Zarà, Marta; Barbieri, Silvia S.; Ieraci, Alessandro

doi:10.1016/j.redox.2024.103060

Redox Biology

2024

DOI: 10.1016/j.redox.2024.103060

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NADPH-oxidases as potential pharmacological targets for thrombosis and depression comorbidity

Patrizia Amadio,

Leonardo Sandrini,

Marta Zarà

et al.

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2024

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Cited by 8 publications

References 325 publications

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Development of New Peptidomimetic NADPH Oxidase Inhibitors with Antithrombotic Properties

Scalia,

Chirco,

Calugi

et al. 2024

ChemMedChem

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The ability of synthetic peptides inhibitors of NOX1 to effectively block the production of ROS by the enzyme was studied with different methodologies. Specifically, taking advantage of our understanding of the active epitope of the regulatory NOX1 subunit NOXA1 as a potent inhibitor of NOX1‐derived O2•‐ formation, a panel of peptidomimetic derivatives of this peptide were designed and synthesized with the aim of improving their activity and increasing their stability in plasma. The results highlighted that improved efficacy and potency was found for both the peptide‐peptoid hybrid GS2, whereas stapled peptide AC5 and its precursor showed higher stability despite lower biological potency. This study showed that minimal structural modifications of NOXA1 peptides are required to improve both their potency and stability to finally achieve best candidates as new potential anti‐thrombotic drugs.

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Development of New Peptidomimetic NADPH Oxidase Inhibitors with Antithrombotic Properties

Scalia,

Chirco,

Calugi

et al. 2024

ChemMedChem

View full text Add to dashboard Cite

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A Machine Learning‐Based Approach for the Prediction of Anticoagulant Activity of Hypericum perforatum L. and Evaluation of Compound Activity

Zhang,

Nie,

Zhang

et al. 2024

Phytochemical Analysis

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IntroductionHypericum perforatum L. (HPL) is extensively researched domestically and internationally as a medicinal plant. However, no reports of studies related to the anticoagulant activity of HPL have been retrieved. The specific bioactive components are unknown.ObjectiveThe aim of this study was to develop a machine learning (ML) method for rapid prediction of anticoagulant activity in HPL and evaluation of compound activity. Materials and methods.First, an in vitro anticoagulant activity assay was developed for the determination of the bioactivity of various medicinal parts of HPL. Then, the peak areas of compounds in HPL were integrated using UPLC‐Q‐TOF‐MS analysis. Subsequently, nine independent ML methods and two ensemble learning methods have been established to predict the anticoagulant activity of HPL and to evaluate the contribution of compounds. Feature importance scores were used for models visualization.ResultsA total of 24 compounds were shown to exhibited superior anticoagulant activity. Molecular docking experiments likewise confirmed this result. The results show that the branches of HPL have excellent anticoagulant activity, which has been previously overlooked. The established ML model demonstrated good performance in the prediction of the activity of HPL.ConclusionThe results were accurate and reliable, which significantly improved the efficiency of active compounds screening, and further exploration in this area is warranted.

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Anti-inflammatory and antioxidant mechanisms of coniferaldehyde in lipopolysaccharide-induced neuroinflammation: Involvement of AMPK/Nrf2 and TAK1/MAPK/NF-κB signaling pathways

Park,

Park

et al. 2024

European Journal of Pharmacology

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NADPH-oxidases as potential pharmacological targets for thrombosis and depression comorbidity

Cited by 8 publications

References 325 publications

Development of New Peptidomimetic NADPH Oxidase Inhibitors with Antithrombotic Properties

Development of New Peptidomimetic NADPH Oxidase Inhibitors with Antithrombotic Properties

A Machine Learning‐Based Approach for the Prediction of Anticoagulant Activity of Hypericum perforatum L. and Evaluation of Compound Activity

Anti-inflammatory and antioxidant mechanisms of coniferaldehyde in lipopolysaccharide-induced neuroinflammation: Involvement of AMPK/Nrf2 and TAK1/MAPK/NF-κB signaling pathways

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