ArticleJournal of medicinal chemistry2018
Insights into the Impact of a Membrane-Anchoring Moiety on the Biological Activities of Bivalent Compounds As Potential Neuroprotectants for Alzheimer's Disease.
Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Enhanced Neuroprotection by Diosgenin and Pterostilbene Combination Against Neurotoxicity Induced by Amyloid-Β 1-42 in SH-SY5Y Differentiated Cell Models.Annals of neurosciences · 2025Article
- Effects of Cholesterol on the Breast Cancer Resistance Protein: Studies through the Synthesis and Biological Evaluation of Chemical Tools.ChemMedChem · 2025Article
- Article
- Antipsychotic effect of diosgenin in ketamine-induced murine model of schizophrenia: Involvement of oxidative stress and cholinergic transmission.IBRO neuroscience reports · 2024Article
- New Insight Into Cardioprotection From Anthracyclines: Still Converging on the Mitochondria.JACC. CardioOncology · 2023Article
- Rosmarinic Acid Potently Detoxifies Amylin Amyloid and Ameliorates Diabetic Pathology in a Transgenic Rat Model of Type 2 Diabetes.ACS pharmacology & translational science · 2021Article
- Structural understanding of 5-(4-hydroxy-phenyl)-N-(2-(5-methoxy-1H-indol-3-yl)-ethyl)-3-oxopentanamide as a neuroprotectant for Alzheimer's disease.Bioorganic & medicinal chemistry letters · 2021Article
- A comparison of the location in membranes of curcumin and curcumin-derived bivalent compounds with potential neuroprotective capacity for Alzheimer's disease.Colloids and surfaces. B, Biointerfaces · 2021Article
- Characterization and Discovery of a Selective Small-Molecule Modulator of Mitochondrial Complex I Targeting a Unique Binding Site.Journal of medicinal chemistry · 2020Article
- Therapeutic Potential of Diosgenin and Its Major Derivatives against Neurological Diseases: Recent Advances.Oxidative medicine and cellular longevity · 2020Review
- Development of bivalent compounds as potential neuroprotectants for Alzheimer's disease.Bioorganic & medicinal chemistry letters · 2019Article
- Design and characterization of bivalent compounds as potential neuroprotectants for Alzheimer's disease: Impact of the spacer on biological activity.Bioorganic & medicinal chemistry letters · 2018Article
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Authors and funding
12 authors.
Funding
Abstract
Bivalent compounds anchoring in different manners to the membrane were designed and biologically characterized to understand the contribution of the anchor moiety to their biological activity as neuroprotectants for Alzheimer's disease. Our results established that the anchor moiety is essential, and we identified a preference for diosgenin, as evidenced by 17MD. Studies in primary neurons and mouse brain mitochondria also identified 17MD as exhibiting activity on neuritic outgrowth and the state 3 oxidative rate of glutamate while preserving the coupling capacity of the mitochondria. Significantly, our studies demonstrated that the integrated bivalent structure is essential to the observed biological activities. Further studies employing bivalent compounds as probes in a model membrane also revealed the influence of the anchor moiety on how they interact with the membrane. Collectively, our results suggest diosgenin to be an optimal anchor moiety, providing bivalent compounds with promising pharmacology that have potential applications for Alzheimer's disease.
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