Biochemical characterization of QPX7728, a new ultrabroad-spectrum beta-lactamase inhibitor of serine and metallo-beta-lactamases

R Tsivkovski, M Totrov… - Antimicrobial agents and …, 2020 - Am Soc Microbiol
ABSTRACT QPX7728 is a new ultrabroad-spectrum inhibitor of serine and metallo-beta-
lactamases (MBLs) from a class of cyclic boronates that gave rise to vaborbactam. The …

Beta-lactamase inhibitors from laboratory to clinic

K Bush - Clinical microbiology reviews, 1988 - Am Soc Microbiol
beta-Lactamases constitute the major defense mechanism of pathogenic bacteria against
beta-lactam antibiotics. When the beta-lactam ring of this antibiotic class is hydrolyzed …

Cyclic boronates inhibit all classes of β-lactamases

ST Cahill, R Cain, DY Wang, CT Lohans… - Antimicrobial agents …, 2017 - Am Soc Microbiol
ABSTRACT β-Lactamase-mediated resistance is a growing threat to the continued use of β-
lactam antibiotics. The use of the β-lactam-based serine-β-lactamase (SBL) inhibitors …

Emerging strategies to combat β-lactamase producing ESKAPE pathogens

CO Vrancianu, I Gheorghe, EG Dobre, IC Barbu… - International journal of …, 2020 - mdpi.com
Since the discovery of penicillin by Alexander Fleming in 1929 as a therapeutic agent
against staphylococci, β-lactam antibiotics (BLAs) remained the most successful antibiotic …

Spectrum of beta-lactamase inhibition by the cyclic boronate QPX7728, an ultrabroad-spectrum beta-lactamase inhibitor of serine and metallo-beta-lactamases …

O Lomovskaya, R Tsivkovski, K Nelson… - Antimicrobial Agents …, 2020 - Am Soc Microbiol
ABSTRACT QPX7728 is an ultrabroad-spectrum boronic acid beta-lactamase inhibitor, with
potent inhibition of key serine and metallo-beta-lactamases being observed in biochemical …

b-Lactamase inhibitors

MGP Page - Drug Resistance Updates, 2000 - Elsevier
The use of β-lactamase inhibitors in combination with a β-lactamase-susceptible antibiotic is
a useful strategy to rescue otherwise good antibiotics from failure. However, recent years …

Pharmacokinetics and pharmacodynamics of β‐lactamase inhibitors

RL Crass, MP Pai - … : The Journal of Human Pharmacology and …, 2019 - Wiley Online Library
Novel β‐lactamase inhibitors have extended the reach of new and existing β‐lactams
against multidrug‐resistant bacteria expressing β‐lactamases. The efficacy of these …

[HTML][HTML] β-Lactamases and β-Lactamase Inhibitors in the 21st Century

CL Tooke, P Hinchliffe, EC Bragginton… - Journal of molecular …, 2019 - Elsevier
The β-lactams retain a central place in the antibacterial armamentarium. In Gram-negative
bacteria, β-lactamase enzymes that hydrolyze the amide bond of the four-membered β …

Kinetics of avibactam inhibition against class A, C, and D β-lactamases

DE Ehmann, H Jahić, PL Ross, RF Gu, J Hu… - Journal of Biological …, 2013 - ASBMB
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 …

Targeting Multidrug-Resistant Acinetobacter spp.: Sulbactam and the Diazabicyclooctenone β-Lactamase Inhibitor ETX2514 as a Novel Therapeutic Agent

MD Barnes, V Kumar, CR Bethel, SH Moussa… - MBio, 2019 - Am Soc Microbiol
Multidrug-resistant (MDR) Acinetobacter spp. poses a significant therapeutic challenge in
part due to the presence of chromosomally encoded β-lactamases, including class C …