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Chem Biol Drug Des ; 87(3): 455-66, 2016 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-26547388

RESUMEN

In this study, quantitative structure-activity relationship studies which make use of molecular dynamics trajectories were performed on a set of 54 glucokinase protein activators. The conformations obtained by molecular dynamics simulation were superimposed according to the twelve alignments tested in a virtual three-dimensional box comprised of 2 Å cells. The models were generated by the technique that combines genetic algorithms and partial least squares. The best alignment models generated with a determination coefficient (r(2)) between 0.674 and 0.743 and cross-validation (q(2)) between 0.509 and 0.610, indicating good predictive capacity. The 4D-QSAR models developed in this study suggest novel molecular regions to be explored in the search for better glucokinase activators.


Asunto(s)
Glucoquinasa/metabolismo , Activación Enzimática , Humanos , Simulación de Dinámica Molecular , Relación Estructura-Actividad Cuantitativa
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