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Mol Pharmacol ; 88(3): 421-7, 2015 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-26078313

RESUMEN

Cytochrome c (cyt c) release from mitochondria is accepted to be the point of no return for eliciting a cascade of interactions that lead to apoptosis. A strategy for containing sustained apoptosis is to reduce the mitochondrial permeability pore opening. Pore opening is enhanced by peroxidase activity of cyt c gained upon its complexation with cardiolipin in the presence of reactive oxygen species. Blocking access to the heme group has been proposed as an effective intervention method for reducing, if not eliminating, the peroxidase activity of cyt c. In the present study, using a combination of druggability simulations, pharmacophore modeling, virtual screening, and in vitro fluorescence measurements to probe peroxidase activity, we identified three repurposable drugs and seven compounds that are validated to effectively inhibit the peroxidase activity of cyt c.


Asunto(s)
Dominio Catalítico , Complejo IV de Transporte de Electrones/química , Inhibidores Enzimáticos/química , Peroxidasas/antagonistas & inhibidores , Bibliotecas de Moléculas Pequeñas/química , Secuencia de Aminoácidos , Complejo IV de Transporte de Electrones/antagonistas & inhibidores , Inhibidores Enzimáticos/farmacología , Humanos , Simulación del Acoplamiento Molecular , Datos de Secuencia Molecular , Peroxidasas/química , Bibliotecas de Moléculas Pequeñas/farmacología
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