Antibiotic resistance breakers: current approaches and future directions

M Laws, A Shaaban, KM Rahman - FEMS microbiology reviews, 2019 - academic.oup.com
Infections of antibiotic-resistant pathogens pose an ever-increasing threat to mankind. The
investigation of novel approaches for tackling the antimicrobial resistance crisis must be part …

An update on β-lactamase inhibitor discovery and development

JD Docquier, S Mangani - Drug Resistance Updates, 2018 - Elsevier
Antibiotic resistance, and the emergence of pan-resistant clinical isolates, seriously
threatens our capability to treat bacterial diseases, including potentially deadly hospital …

Discovery of taniborbactam (VNRX-5133): a broad-spectrum serine-and metallo-β-lactamase inhibitor for carbapenem-resistant bacterial infections

B Liu, REL Trout, GH Chu, D McGarry, RW Jackson… - 2019 - ACS Publications
A major resistance mechanism in Gram-negative bacteria is the production of β-lactamase
enzymes. Originally recognized for their ability to hydrolyze penicillins, emergent β …

Discovery of cyclic boronic acid QPX7728, an ultrabroad-spectrum inhibitor of serine and metallo-β-lactamases

SJ Hecker, KR Reddy, O Lomovskaya… - Journal of medicinal …, 2020 - ACS Publications
Despite major advances in the β-lactamase inhibitor field, certain enzymes remain refractory
to inhibition by agents recently introduced. Most important among these are the class B …

Discovery of a cyclic boronic acid β-lactamase inhibitor (RPX7009) with utility vs class A serine carbapenemases

SJ Hecker, KR Reddy, M Totrov, GC Hirst… - 2015 - ACS Publications
The increasing dissemination of carbapenemases in Gram-negative bacteria has threatened
the clinical usefulness of the β-lactam class of antimicrobials. A program was initiated to …

Bicyclic boronate VNRX-5133 inhibits metallo-and serine-β-lactamases

A Krajnc, J Brem, P Hinchliffe, K Calvopiña… - Journal of Medicinal …, 2019 - ACS Publications
The bicyclic boronate VNRX-5133 (taniborbactam) is a new type of β-lactamase inhibitor in
clinical development. We report that VNRX-5133 inhibits serine-β-lactamases (SBLs) and …

β-Lactamase inhibitors to restore the efficacy of antibiotics against superbugs

C Gonzalez-Bello, D Rodríguez, M Pernas… - Journal of medicinal …, 2019 - ACS Publications
Infections caused by resistant bacteria are nowadays too common, and some pathogens
have even become resistant to multiple types of antibiotics, in which case few or even no …

Boron containing compounds as protease inhibitors

R Smoum, A Rubinstein, VM Dembitsky… - Chemical …, 2012 - ACS Publications
Proteases form one of the largest and more important groups of enzymes. They selectively
catalyze the hydrolysis of peptide bonds and can be divided into four major classes …

Structural basis of metallo-β-lactamase, serine-β-lactamase and penicillin-binding protein inhibition by cyclic boronates

J Brem, R Cain, S Cahill, MA McDonough… - Nature …, 2016 - nature.com
Abstract β-Lactamases enable resistance to almost all β-lactam antibiotics. Pioneering work
revealed that acyclic boronic acids can act as 'transition state analogue'inhibitors of …

Pharmaceutical approaches to target antibiotic resistance mechanisms

D Schillaci, V Spanò, B Parrino… - Journal of medicinal …, 2017 - ACS Publications
There is urgent need for new therapeutic strategies to fight the global threat of antibiotic
resistance. The focus of this Perspective is on chemical agents that target the most common …