Structure- and Ligand-Dynamics-Based Design of Novel Antibiotics Targeting Lipid A Enzymes LpxC and LpxH in Gram-Negative Bacteria

Two Distinct Mechanisms of Inhibition of LpxA Acyltransferase Essential for Lipopolysaccharide Biosynthesis

(2020) Wooseok Han et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Structural basis of the UDP-diacylglucosamine pyrophosphohydrolase LpxH inhibition by sulfonyl piperazine antibiotics

(2020) Jae Cho et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Unrecognized Threat of Secondary Bacterial Infections with COVID-19

(2020) Mylene Vaillancourt et al.   mBio

Synthesis and evaluation of sulfonyl piperazine LpxH inhibitors

(2020) Seung-Hwa Kwak et al.   BIOORGANIC CHEMISTRY

Lead optimization of 2-hydroxymethyl imidazoles as non-hydroxamate LpxC inhibitors: Discovery of TP0586532

(2020) Fumihito Ushiyama et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Fragment-Based Discovery of Novel Non-Hydroxamate LpxC Inhibitors with Antibacterial Activity

(2020) Yousuke Yamada et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure–Activity Relationship of Sulfonyl Piperazine LpxH Inhibitors Analyzed by an LpxE-Coupled Malachite Green Assay

(2019) Minhee Lee et al.   ACS Infectious Diseases

Optimization of LpxC Inhibitors for Antibacterial Activity and Cardiovascular Safety

(2019) Frederick Cohen et al.   ChemMedChem

Structural and Biological Basis of Small Molecule Inhibition of Escherichia coli LpxD Acyltransferase Essential for Lipopolysaccharide Biosynthesis

(2019) Xiaolei Ma et al.   ACS Infectious Diseases

Antisense inhibition of lpxB gene expression in Acinetobacter baumannii by peptide–PNA conjugates and synergy with colistin

(2019) Marta Martínez-Guitián et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Discovery of dual-activity small-molecule ligands of Pseudomonas aeruginosa LpxA and LpxD using SPR and X-ray crystallography

(2019) Kyle G. Kroeck et al.   Scientific Reports

The substrate-binding cap of the UDP-diacylglucosamine pyrophosphatase LpxH is highly flexible, enabling facile substrate binding and product release

(2018) Thomas E. Bohl et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Towards Understanding MCR-like Colistin Resistance

(2018) Jian Sun et al.   TRENDS IN MICROBIOLOGY

The global distribution and spread of the mobilized colistin resistance gene mcr-1

(2018) Ruobing Wang et al.   Nature Communications

LpxC inhibitors: a patent review (2010-2016)

(2017) Dmitrii V. Kalinin et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Curative Treatment of Severe Gram-Negative Bacterial Infections by a New Class of Antibiotics Targeting LpxC

(2017) Nadine Lemaître et al.   mBio

LpxK Is Essential for Growth of Acinetobacter baumannii ATCC 19606: Relationship to Toxic Accumulation of Lipid A Pathway Intermediates

(2017) Jun-Rong Wei et al.   mSphere

High susceptibility of MDR and XDR Gram-negative pathogens to biphenyl-diacetylene-based difluoromethyl-allo-threonyl-hydroxamate LpxC inhibitors

(2016) Marie Titecat et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Emergence of plasmid-mediated colistin resistance mechanism MCR-1 in animals and human beings in China: a microbiological and molecular biological study

(2016) Yi-Yun Liu et al.   LANCET INFECTIOUS DISEASES

Discovery of the Elusive UDP-Diacylglucosamine Hydrolase in the Lipid A Biosynthetic Pathway in Chlamydia trachomatis

(2016) Hayley E. Young et al.   mBio

Drug design from the cryptic inhibitor envelope

(2016) Chul-Jin Lee et al.   Nature Communications

Antibacterial Drug Discovery Targeting the Lipopolysaccharide Biosynthetic Enzyme LpxC

(2016) Alice L. Erwin   Cold Spring Harbor Perspectives in Medicine

Structure of the essential Haemophilus influenzae UDP-diacylglucosamine pyrophosphohydrolase LpxH in lipid A biosynthesis

(2016) Jae Cho et al.   Nature Microbiology

Toxic Accumulation of LPS Pathway Intermediates Underlies the Requirement of LpxH for Growth of Acinetobacter baumannii ATCC 19606

(2016) Daryl L. Richie et al.   PLoS One

Crystal structures of the UDP-diacylglucosamine pyrophosphohydrase LpxH from Pseudomonas aeruginosa

(2016) Chiaki Okada et al.   Scientific Reports

Novel Antibacterial Targets and Compounds Revealed by a High-Throughput Cell Wall Reporter Assay

(2015) Asha S. Nayar et al.   JOURNAL OF BACTERIOLOGY

Biosynthesis and Export of Bacterial Lipopolysaccharides

(2014) Chris Whitfield et al.   Annual Review of Biochemistry

LpxC Inhibitors as New Antibacterial Agents and Tools for Studying Regulation of Lipid A Biosynthesis in Gram-Negative Pathogens

(2014) A. P. Tomaras et al.   mBio

Structural Basis of the Promiscuous Inhibitor Susceptibility of Escherichia coli LpxC

(2013) Chul-Jin Lee et al.   ACS Chemical Biology

The UDP-diacylglucosamine Pyrophosphohydrolase LpxH in Lipid A Biosynthesis Utilizes Mn2+Cluster for Catalysis

(2013) Hayley E. Young et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Synthesis, Structure, and Antibiotic Activity of Aryl-Substituted LpxC Inhibitors

(2013) Xiaofei Liang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Combination Therapy for Treatment of Infections with Gram-Negative Bacteria

(2012) P. D. Tamma et al.   CLINICAL MICROBIOLOGY REVIEWS

LpxI structures reveal how a lipid A precursor is synthesized

(2012) Louis E Metzger et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Colistin Resistance in Acinetobacter baumannii Is Mediated by Complete Loss of Lipopolysaccharide Production

(2010) J. H. Moffatt et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

An Alternative Route for UDP-Diacylglucosamine Hydrolysis in Bacterial Lipid A Biosynthesis

(2010) Louis E. Metzger et al.   BIOCHEMISTRY

Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold

(2010) Xiaofei Liang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Species-Specific and Inhibitor-Dependent Conformations of LpxC: Implications for Antibiotic Design

(2010) Chul-Jin Lee et al.   CHEMISTRY & BIOLOGY

Active Site Metal Ion in UDP-3-O-((R)-3-Hydroxymyristoyl)-N-acetylglucosamine Deacetylase (LpxC) Switches between Fe(II) and Zn(II) Depending on Cellular Conditions

(2010) Samuel G. Gattis et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Steady-State Kinetics and Mechanism of LpxD, theN-Acyltransferase of Lipid A Biosynthesis†

(2008) Craig M. Bartling et al.   BIOCHEMISTRY

Bad Bugs, No Drugs: No ESKAPE! An Update from the Infectious Diseases Society of America

(2008) Helen W. Boucher et al.   CLINICAL INFECTIOUS DISEASES