[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 …

Metallo-β-lactamases in the age of multidrug resistance: from structure and mechanism to evolution, dissemination, and inhibitor design

G Bahr, LJ Gonzalez, AJ Vila - Chemical reviews, 2021 - ACS Publications
Antimicrobial resistance is one of the major problems in current practical medicine. The
spread of genes coding for resistance determinants among bacteria challenges the use of …

Metallo-β-lactamases: structure, function, epidemiology, treatment options, and the development pipeline

SE Boyd, DM Livermore, DC Hooper… - Antimicrobial agents …, 2020 - Am Soc Microbiol
Modern medicine is threatened by the global rise of antibiotic resistance, especially among
Gram-negative bacteria. Metallo-β-lactamase (MBL) enzymes are a particular concern and …

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 …

The boron advantage: the evolution and diversification of boron's applications in medicinal chemistry

K Messner, B Vuong, GK Tranmer - Pharmaceuticals, 2022 - mdpi.com
In this review, the history of boron's early use in drugs, and the history of the use of boron
functional groups in medicinal chemistry applications are discussed. This includes …

Antibiotic adjuvants: a versatile approach to combat antibiotic resistance

G Dhanda, Y Acharya, J Haldar - ACS omega, 2023 - ACS Publications
The problem of antibiotic resistance is on the rise, with multidrug-resistant strains emerging
even to the last resort antibiotics. The drug discovery process is often stalled by stringent cut …

Targeting metalloenzymes for therapeutic intervention

AY Chen, RN Adamek, BL Dick, CV Credille… - Chemical …, 2018 - ACS Publications
Metalloenzymes are central to a wide range of essential biological activities, including
nucleic acid modification, protein degradation, and many others. The role of metalloenzymes …

VNRX-5133 (Taniborbactam), a Broad-Spectrum Inhibitor of Serine- and Metallo-β-Lactamases, Restores Activity of Cefepime in Enterobacterales and Pseudomonas …

JC Hamrick, JD Docquier, T Uehara… - Antimicrobial Agents …, 2020 - Am Soc Microbiol
As shifts in the epidemiology of β-lactamase-mediated resistance continue, carbapenem-
resistant Enterobacterales (CRE) and carbapenem-resistant Pseudomonas aeruginosa …

The versatility of boron in biological target engagement

DB Diaz, AK Yudin - Nature Chemistry, 2017 - nature.com
Boron-containing molecules have been extensively used for the purposes of chemical
sensing, biological probe development and drug discovery. Due to boron's empty p orbital, it …

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 …