High-Resolution X-ray Structure of an Acyl-Enzyme Species for the Class D OXA-10 β-Lactamase

• DOI: 10.1021/ja016736t
• Publication Date: 2002-07-26T04:49:41Z
• Authors: Laurent Maveyraud; Dasantila Golemi-...; Akihiro Ishiwata; Oussama Meroueh; Shahriar Mobashery; Jean-Pierre Samama
• Keywords: Models, Molecular; 0301 basic medicine; Kinetics; 03 medical and health sciences; Protein Conformation; Hydrogen-Ion Concentration; Crystallography, X-Ray; beta-Lactamase Inhibitors; Nuclear Magnetic Resonance, Biomolecular; beta-Lactamases; 3. Good health

Beta-lactamases are resistance enzymes for beta-lactam antibiotics. These enzymes hydrolyze the beta-lactam moieties of these antibiotics, rendering them inactive. Of the four classes of known beta-lactamases, the enzymes of class D are the least understood. We report herein the high-resolution (1.9 A) crystal structure of the class D OXA-10 beta-lactamase inhibited by a penicillanate derivative. The structure provides evidence that the carboxylated Lys-70 (a carbamate) is intimately involved in the mechanism of the enzyme.