Artículo

A minimalistic approach to identify substrate binding features in B1 Metallo-β-lactamases

Poeylaut Palena, Andrés AlbertoIcon ; Tomatis, Pablo EmilianoIcon ; Karsisiotis, Andreas I.; Damblon, Christian; Mata, Ernesto GabinoIcon ; Vila, Alejandro JoseIcon
Fecha de publicación: 15/09/2007
Editorial: Elsevier
Revista: Biorganic and Medicinal Chemistry Letters
ISSN: 0960-894X
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:

Resumen

The 2-oxoazetidinylacetate sodium salt was synthesized as a model of a minimal β-lactam drug. This compound and the monobactam aztreonam were assayed as substrates of the Metallo-β-lactamase BcII. None of them was hydrolyzed by the enzyme. While the azetidinone was not able to bind BcII, aztreonam was shown to bind in a nonproductive mode. These results provide an explanation for the unability of Metallo-β-lactamases to inactive monobactams and give some clues for inhibitor design.
Palabras clave: Metallo-beta-lactamase , Inhibitor design , Ligand binding , Monocyclic β-lactams
 
Archivos asociados
Thumbnail
 
Tamaño: 234.1Kb
Formato: PDF
.
Licencia
info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)
Identificadores
URI: http://hdl.handle.net/11336/155055
DOI: http://dx.doi.org/10.1016/j.bmcl.2007.06.089
URL: https://www.sciencedirect.com/science/article/pii/S0960894X07007962
Colecciones
Articulos(IBR)
Articulos de INST.DE BIOLOGIA MOLECULAR Y CELULAR DE ROSARIO
Articulos(IQUIR)
Articulos de INST.DE QUIMICA ROSARIO
Citación
Poeylaut Palena, Andrés Alberto; Tomatis, Pablo Emiliano; Karsisiotis, Andreas I.; Damblon, Christian; Mata, Ernesto Gabino; et al.; A minimalistic approach to identify substrate binding features in B1 Metallo-β-lactamases; Elsevier; Biorganic and Medicinal Chemistry Letters; 17; 18; 15-9-2007; 5171-5174
Compartir
Altmétricas