INVESTIGADORES
TOMATIS Pablo Emiliano
artículos
Título:
A minimalistic approach to identify substrate binding features in B1 Metallo-b-lactamases
Autor/es:
ANDRES A. POEYLAUT-PALENA; PABLO E. TOMATIS; ANDREAS I. KARSISIOTIS; CHRISTIAN DAMBLON; ERNESTO G. MATA; ALEJANDRO J. VILA
Revista:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Referencias:
Año: 2007
ISSN:
0960-894X
Resumen:
The 2oxoazetidinylacetate sodium salt was synthesized as a model of a minimal βlactam drug. This compound and the monobactam aztreonam were assayed as substrates of the Metalloβlactamase 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 non productive mode. These results provide an explanation for the unability of Metalloβlactamases to inactive monobactams and give some clues for inhibitor design.