Homology Modeling and Blind Docking Approach Studies of Pig Heart Fumarase

The fumarase is an enzyme that could be used as target indrug design to treat infections by Helicobacter pylori andTrypanosoma brucei. In the first step, homology modeling wasemployed to build the 3D structure of pig heart fumarase (FUM P).Then, Q-Site Finder program was used to identify the potenti...

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Detalles Bibliográficos
Autores: Martha Cecilia Rosales, José Trujillo Ferrara, José Correa Basurto
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2007
País:México
Institución:Instituto Politécnico Nacional
Repositorio:Redalyc-IPN
OAI Identifier:oai:redalyc.org:47551305
Acceso en línea:https://www.redalyc.org/articulo.oa?id=47551305
Access Level:acceso abierto
Palabra clave:Multidisciplinaria (Ciencias Naturales y Exactas)
docking
Homology
arylderivatives
pig heart fumarase
Descripción
Sumario:The fumarase is an enzyme that could be used as target indrug design to treat infections by Helicobacter pylori andTrypanosoma brucei. In the first step, homology modeling wasemployed to build the 3D structure of pig heart fumarase (FUM P).Then, Q-Site Finder program was used to identify the potential bindingsites of FUM P and fumarase of Saccharomyces cerevisiae (FUMY). Further, molecular docking of arylderivatives substituted at thearomatic ring with an electron withdrawing or donating groups wereevaluated on FUM P and on FUM Y to validate the homology model.The homology model of FUM P showed a structure very similar(70.33 % of identity in sequence) to the crystal structure of FUM Y.Some active sites were identified by Q-Site Finder server on FUM Pand on FUM Y which could correspond to sites A and B. The dockingresults showed that some compounds were bonded at the site Aon FUM P and FUM Y being those with electron withdrawing groupswith more affinity on FUM P, suggesting that electronic effects arethe more important ones during the recognition process by FUM P.