Identification of New Snake Venom Metalloproteinase Inhibitors Using Compound Screening and Rational Peptide Design

 

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Detalles Bibliográficos
Autores: Villalta Romero, Fabián, Gortat, Anna, Herrera, Andrés E., Arguedas, Rebeca, Quesada Espinoza, Francisco Javier, Lopes de Melo, Robson, Calvete Chornet, Juan José, Montero Villalobos, Mavis Lili, Murillo Masís, Renato, Rucavado Romero, Alexandra, Pérez Payá, Enrique
Formato: artículo original
Fecha de Publicación:2012
Descripción:The majority of snakebite envenomations in Central America are caused by the viperid species Bothrops asper, whose venom contains a high proportion of zinc-dependent metalloproteinases that play a relevant role in the pathogenesis of hemorrhage characteristic of these envenomations. Broad metalloproteinase inhibitors, such as the peptidomimetic hydroxamate Batimastat, have been shown to inhibit snake venom metalloproteinases (SVMP). However, the difficulty in having open public access to Batimastat and similar molecules highlights the need to design new inhibitors of SVMPs that could be applied in the treatment of snakebite envenomations. We have chosen the SVMP BaP1 as a model to search for new inhibitors using different strategies, that is, screening of the Prestwick Chemical Library and rational peptide design. Results from these approaches provide clues on the structural requirements for efficient BaP1 inhibition and pave the way for the design of new inhibitors of SVMP.
País:Kérwá
Institución:Universidad de Costa Rica
Repositorio:Kérwá
OAI Identifier:oai:https://www.kerwa.ucr.ac.cr:10669/29627
Acceso en línea:http://pubs.acs.org/doi/abs/10.1021/ml300068r
https://hdl.handle.net/10669/29627
Access Level:acceso abierto
Palabra clave:BaP1
Metalloproteinase inhibitors
Protein docking
Snake venom
Metalloproteinases