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  • Multidirectional in vitro and in cellulo studies as a tool for identification of multi-target-directed ligands aiming at symptoms and causes of Alzheimer's disease [Elektronski vir]
    Szałaj, Natalia ...
    Effective therapy of Alzheimer's disease (AD) requires treatment with a combination of drugs that modulate various pathomechanisms contributing to the disease. In our research, we have focused on the ... development of multi-target-directed ligands - 5-HT6 receptor antagonists and cholinesterase inhibitors - with disease-modifying properties. We have performed extended in vitro (FRET assay) and in cellulo (Escherichia coli model of protein aggregation) studies on their [beta]-secretase, tau, and amyloid - aggregation inhibitory activity. Within these multifunctional ligands, we have identified compound 17 with inhibitory potency against tau and amyloid - aggregation in in cellulo assay of 59% and 56% at 10 [micro]M, respectively, hBACE IC50=4 [micro]M, h5TH6 K i=94%nM, hAChE IC50=26%nM, and eqBuChE IC50=5%nM. This study led to the development of multifunctional ligands with a broad range of biological activities crucial not only for the symptomatic but also for the disease-modifying treatment of AD.
    Vir: Journal of enzyme inhibition and medicinal chemistry. - ISSN 1475-6374 (Vol. 35, iss. 1, 2020, str. 1944-1952)
    Vrsta gradiva - e-članek ; neleposlovje za odrasle
    Leto - 2020
    Jezik - angleški
    COBISS.SI-ID - 36188163

    Povezava(-e):

    https://www.tandfonline.com/doi/full/10.1080/14756366.2020.1835882
    DOI

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