13C-Carbamylation as a mechanistic probe for the inhibition of class D β-lactamases by avibactam and halide ions
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چکیده
منابع مشابه
Kinetics of avibactam inhibition against Class A, C, and D β-lactamases.
Avibactam is a non-β-lactam β-lactamase inhibitor with a spectrum of activity that includes β-lactamase enzymes of classes A, C, and selected D examples. In this work acylation and deacylation rates were measured against the clinically important enzymes CTX-M-15, KPC-2, Enterobacter cloacae AmpC, Pseudomonas aeruginosa AmpC, OXA-10, and OXA-48. The efficiency of acylation (k2/Ki) varied across ...
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β-Lactamases are the most important mechanisms of resistance to the β-lactam antibacterials. There are two mechanistic classes of β-lactamases: the serine β-lactamases (SBLs) and the zinc-dependent metallo-β-lactamases (MBLs). Avibactam, the first clinically useful non-β-lactam β-lactamase inhibitor, is a broad-spectrum SBL inhibitor, which is used in combination with a cephalosporin antibiotic...
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The Class D β-lactamases have emerged as a prominent resistance mechanism against β-lactam antibiotics that previously had efficacy against infections caused by pathogenic bacteria, especially by Acinetobacter baumannii and the Enterobacteriaceae. The phenotypic and structural characteristics of these enzymes correlate to activities that are classified either as a narrow spectrum, an extended s...
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β-Lactamase inhibition is an important clinical strategy in overcoming β-lactamase-mediated resistance to β-lactam antibiotics in Gram negative bacteria. A new β-lactamase inhibitor, avibactam, is entering the clinical arena and promising to be a major step forward in our antibiotic armamentarium. Avibactam has remarkable broad-spectrum activity in being able to inhibit classes A, C, and some c...
متن کاملInhibition of Class D -Lactamases by Acyl Phosphates and Phosphonates
The resistance of bacteria to -lactam antibiotics is to a large extent due to -lactamases (14). There is a wide range of -lactamases, although from a structural standpoint, they can be divided into four classes, A, B, C, and D (11). Each class contains many variants of widely differing substrate specificities and thus clinical importance. Of the canonical four classes, it is perhaps class D tha...
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ژورنال
عنوان ژورنال: Organic & Biomolecular Chemistry
سال: 2017
ISSN: 1477-0520,1477-0539
DOI: 10.1039/c7ob01514c