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J Biomol Struct Dyn ; 32(10): 1601-12, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-23998201

RESUMEN

Smallpox was one of the most devastating diseases in the human history and still represents a serious menace today due to its potential use by bioterrorists. Considering this threat and the non-existence of effective chemotherapy, we propose the enzyme thymidylate kinase from Variola virus (VarTMPK) as a potential target to the drug design against smallpox. We first built a homology model for VarTMPK and performed molecular docking studies on it in order to investigate the interactions with inhibitors of Vaccinia virus TMPK (VacTMPK). Subsequently, molecular dynamics (MD) simulations of these compounds inside VarTMPK and human TMPK (HssTMPK) were carried out in order to select the most promising and selective compounds as leads for the design of potential VarTMPK inhibitors. Results of the docking and MD simulations corroborated to each other, suggesting selectivity towards VarTMPK and, also, a good correlation with the experimental data.


Asunto(s)
Modelos Moleculares , Nucleósido-Fosfato Quinasa/química , Viruela/prevención & control , Virus de la Viruela/enzimología , Secuencia de Aminoácidos , Aminoácidos/metabolismo , Sitios de Unión , Bromodesoxiuridina/metabolismo , Humanos , Enlace de Hidrógeno/efectos de los fármacos , Interacciones Hidrofóbicas e Hidrofílicas/efectos de los fármacos , Simulación del Acoplamiento Molecular , Datos de Secuencia Molecular , Nucleósido-Fosfato Quinasa/antagonistas & inhibidores , Inhibidores de Proteínas Quinasas/química , Inhibidores de Proteínas Quinasas/farmacología , Alineación de Secuencia , Homología de Secuencia de Aminoácido , Termodinámica , Virus de la Viruela/efectos de los fármacos
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