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ACS Chem Neurosci ; 15(15): 2795-2810, 2024 Aug 07.
Artículo en Inglés | MEDLINE | ID: mdl-38991155

RESUMEN

The escalating prevalence of Parkinson's disease (PD) underscores the need for innovative therapeutic interventions since current palliative measures, including the standard l-Dopa formulations, face challenges of tolerance and side effects while failing to address the underlying neurodegenerative processes. Here, we introduce DAD9, a novel conjugate molecule that aims to combine symptomatic relief with disease-modifying strategies for PD. Crafted through knowledge-guided chemistry, the molecule combines a nonantibiotic doxycycline derivative with dopamine, preserving neuroprotective attributes while maintaining dopaminergic agonism. This compound exhibited no off-target effects on PD-relevant cell functions and sustained antioxidant and anti-inflammatory properties of the tetracycline precursor. Furthermore, it effectively interfered with the formation and seeding of toxic α-synuclein aggregates without producing detrimental oxidative species. In addition, DAD9 was able to activate dopamine receptors, and docking simulations shed light onto the molecular details of this interaction. These findings position DAD9 as a potential neuroprotective dopaminergic agonist, promising advancements in PD therapeutics.


Asunto(s)
Dopamina , Diseño de Fármacos , Fármacos Neuroprotectores , Enfermedad de Parkinson , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/síntesis química , Fármacos Neuroprotectores/química , Enfermedad de Parkinson/tratamiento farmacológico , Enfermedad de Parkinson/metabolismo , Humanos , Dopamina/metabolismo , alfa-Sinucleína/metabolismo , alfa-Sinucleína/efectos de los fármacos , Doxiciclina/farmacología , Doxiciclina/síntesis química , Agonistas de Dopamina/farmacología , Agonistas de Dopamina/síntesis química , Simulación del Acoplamiento Molecular , Animales
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