Outsmarting metallo-β-lactamases by mimicking their natural evolution

P Oelschlaeger - Journal of inorganic biochemistry, 2008 - Elsevier
Metallo-β-lactamases (MBLs) confer antibiotic resistance to bacteria by hydrolyzing and thus
inactivating β-lactam antibiotics. They have raised concerns due to their broad substrate …

Optimization of amino acid thioesters as inhibitors of metallo-β-lactamase L1

XL Liu, KW Yang, YJ Zhang, Y Ge, Y Xiang… - Bioorganic & Medicinal …, 2016 - Elsevier
The emergence of antibiotic resistance caused by metallo-β-lactamases (MβLs) is a global
public health problem. Recently, we found amino acid thioesters to be a highly promising …

Discovery of a novel covalent non-β-lactam inhibitor of the metallo-β-lactamase NDM-1

T Christopeit, A Albert, HKS Leiros - Bioorganic & medicinal chemistry, 2016 - Elsevier
The inhibition of metallo-β-lactamases (MBL) can prevent the hydrolysis of β-lactam
antibiotics and hence is a promising strategy for the treatment of antibiotic resistant …

An update on the status of potent inhibitors of metallo-β-lactamases

NU Islam - Scientia pharmaceutica, 2013 - mdpi.com
The production of metallo-β-lactamases is the most important strategy by which pathogenic
bacteria become resistant to currently known β-lactam antibiotics. The emergence of these …

The structure of the metallo-β-lactamase VIM-2 in complex with a triazolylthioacetamide inhibitor

T Christopeit, KW Yang, SK Yang… - … Section F: Structural …, 2016 - journals.iucr.org
The increasing number of pathogens expressing metallo-β-lactamases (MBLs), and in this
way achieving resistance to β-lactam antibiotics, is a significant threat to global public …

Structural insights into the subclass B3 metallo-β-lactamase SMB-1 and the mode of inhibition by the common metallo-β-lactamase inhibitor mercaptoacetate

J Wachino, Y Yamaguchi, S Mori… - Antimicrobial agents …, 2013 - Am Soc Microbiol
ABSTRACT A novel subclass B3 metallo-β-lactamase (MBL), SMB-1, recently identified from
a Serratia marcescens clinical isolate, showed a higher hydrolytic activity against a wide …

Targeting clinically-relevant metallo-β-lactamases: from high-throughput docking to broad-spectrum inhibitors

M Brindisi, S Brogi, S Giovani, S Gemma… - Journal of Enzyme …, 2016 - Taylor & Francis
Abstract Metallo-β-lactamases (MBLs) represent one of the most important and widespread
mechanisms of resistance to β-lactam antibiotics (including the life-saving carbapenems) …

Bisthiazolidines: a substrate-mimicking scaffold as an inhibitor of the NDM-1 carbapenemase

MM González, M Kosmopoulou, MF Mojica… - ACS infectious …, 2015 - ACS Publications
Pathogenic Gram-negative bacteria resistant to almost all β-lactam antibiotics are a major
public health threat. Zn (II)-dependent or metallo-β-lactamases (MBLs) produced by these …

NOTA: a potent metallo-β-lactamase inhibitor

AM Somboro, D Tiwari, LA Bester… - Journal of …, 2015 - academic.oup.com
Sir, b-Lactams are the most widely employed antibiotics with their successful use in the
treatment of infectious diseases being well documented for many years. 1 Bacterial …

Irreversible inhibition of metallo‐β‐lactamase (IMP‐1) by 3‐(3‐mercaptopropionylsulfanyl) propionic acid pentafluorophenyl ester

H Kurosaki, Y Yamaguchi, T Higashi… - Angewandte Chemie …, 2005 - Wiley Online Library
Pathogenic bacteria that produce metallo-b-lactamases (MBLs) are emerging as a new
challenge to the medical community. These enzymes catalyze the hydrolysis of a wide …