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

AA Poeylaut-Palena, PE Tomatis, AI Karsisiotis…

Index: Poeylaut-Palena, Andres A.; Tomatis, Pablo E.; Karsisiotis, Andreas I.; Damblon, Christian; Mata, Ernesto G.; Vila, Alejandro J. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 18 p. 5171 - 5174

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Citation Number: 21

Abstract

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 ...