A protein structure-guided covalent scaffold selectively targets the B1 and B2 subclass metallo-β-lactamases. Issue 38 (24th April 2018)

• Record Type: Journal Article
• Authors: Chen, Cheng; Xiang, Yang; Yang, Ke-Wu; Zhang, Yuejuan; Wang, Wen-Ming; Su, Jian-Peng; Ge, Ying; Liu, Ya
• Is Part Of: Chemical communications. Volume 54:Issue 38(2018)
• Page Start: 4802
• Page End: 4805
• Publication Date: 2018-04-24
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/c8cc01067f
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : We report the discovery of ebselen-based dual covalent inhibitors of metallo-β-lactamases. Abstract : We report the discovery of ebselen-based dual covalent inhibitors of metallo-β-lactamases. Fluorescence and MALDI-TOF analysis suggested that the scaffold could bind to NDM-1 by forming a S–Se bond with Cys221 and an amide bond with Lys224 of NDM-1, thereby exhibiting selective inhibition and labeling against B1 and B2 subclass enzymes in vitro and in vivo .