CANADIAN MACROMOLECULAR CRYSTALLOGRAPHY FACILITY

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Research Highlights

DEVELOPING NEW ANTIBIOTICS

A struggle to overcome antibiotic resistance using informed design of novel inhibitors...

Sept. 19, 2012

β-lactams are an important class of antibiotics that includes penicillins and carbapenems. A readily-transferable antibiotic resistance factor called New Delhi metallo-β-lactamase-1 (NDM-1) has been found in enteric bacteria. It confers resistance to β-lactams including some critical antibiotics that are presently considered to be the "last line of defence" against multi-drug resistant Gram negative bacteria. The most clinically significant of these lactamases have 2 active site Zn ions. Researchers have used data collected at the CMCF to describe the details of how β-lactam antibiotics are recognized by these Zn-containing enzymes, including a crystal structure having a potential inhibitor bound.

J. Am. Chem. Soc. 134(28), 11362-11365