Inhibition ofAcinetobacter-Derived Cephalosporinase: Exploring the Carboxylate Recognition Site Using Novel β-Lactamase Inhibitors
نویسندگان
چکیده
منابع مشابه
Biochemical and Structural Analysis of Inhibitors Targeting the ADC-7 Cephalosporinase of Acinetobacter baumannii
β-Lactam resistance in Acinetobacter baumannii presents one of the greatest challenges to contemporary antimicrobial chemotherapy. Much of this resistance to cephalosporins derives from the expression of the class C β-lactamase enzymes, known as Acinetobacter-derived cephalosporinases (ADCs). Currently, β-lactamase inhibitors are structurally similar to β-lactam substrates and are not effective...
متن کاملValidation of the AmpC β-Lactamase Binding Site and Identification of Inhibitors with Novel Scaffolds
AmpC β-lactamase confers resistance to β-lactam antibiotics in multiple Gram-negative bacteria. Therefore, identification of non-β-lactam compounds that inhibit the enzyme is considered crucial to the development of novel antibacterial therapies. Given the highly solvent-exposed active site, it is important to study the induced-fit movements and water-mediated interactions to improve docking ac...
متن کاملComparative Analysis and Identification of Novel Β-lactamase Inhibitors
β-lactam antibiotics are a broad class of antibiotics, consisting of all antibiotic agents that contain a β-lactam nucleus in its molecular structure. Till now β-lactams like penicillins, cephalosporins, monobactams, and carbapenems have been developed. Resistance to various β-lactam antibiotics among target pathogens were started with its first use.The most widespread and important cause is th...
متن کاملA kinetic analysis of the inhibition of FOX-4 β-lactamase, a plasmid-mediated AmpC cephalosporinase, by monocyclic β-lactams and carbapenems.
OBJECTIVES Class C β-lactamases are prevalent among Enterobacteriaceae; however, these enzymes are resistant to inactivation by commercially available β-lactamase inhibitors. In order to find novel scaffolds to inhibit class C β-lactamases, the comparative efficacy of monocyclic β-lactam antibiotics (aztreonam and the siderophore monosulfactam BAL30072), the bridged monobactam β-lactamase inhib...
متن کاملUse of β-Lactam/β-Lactamase Inhibitors for Extended-Spectrum-β-Lactamase Infections: Defining the Right Patient Population.
In a multicenter, multinational observational study that included neutropenic patients with bloodstream infections by extended-spectrum-β-lactamase-producing species, Gudiol et al. (Antimicrob. Agents Chemother. 61:e00164-17, 2017, https://doi.org/10.1128/AAC.00164-17) demonstrated that β-lactam/β-lactamase inhibitors are effective treatment options. A review of this work, however, reminds us t...
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ژورنال
عنوان ژورنال: ACS Infectious Diseases
سال: 2017
ISSN: 2373-8227,2373-8227
DOI: 10.1021/acsinfecdis.7b00153