Targeting Antibiotic Resistance

Discovery of Efficacious Pseudomonas aeruginosa-Targeted Siderophore-Conjugated Monocarbams by Application of a Semi-mechanistic Pharmacokinetic/Pharmacodynamic Model

(2015) Kerry E. Murphy-Benenato et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases

(2015) Scott J. Hecker et al.   JOURNAL OF MEDICINAL CHEMISTRY

Total Syntheses and Initial Evaluation of [Ψ[C(═S)NH]Tpg4]vancomycin, [Ψ[C(═NH)NH]Tpg4]vancomycin, [Ψ[CH2NH]Tpg4]vancomycin, and Their (4-Chlorobiphenyl)methyl Derivatives: Synergistic Binding Pocket and Peripheral Modifications for the Glycopeptide Antibiotics

(2015) Akinori Okano et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A new antibiotic kills pathogens without detectable resistance

(2015) Losee L. Ling et al.   NATURE

Structural and Molecular Basis for Resistance to Aminoglycoside Antibiotics by the Adenylyltransferase ANT(2″)-Ia

(2015) Georgina Cox et al.   mBio

SAR and Structural Analysis of Siderophore-Conjugated Monocarbam Inhibitors of Pseudomonas aeruginosa PBP3

(2015) Kerry E. Murphy-Benenato et al.   ACS Medicinal Chemistry Letters

4,5-Disubstituted 6-Aryloxy-1,3-dihydrobenzo[c][1,2]oxaboroles Are Broad-Spectrum Serine β-Lactamase Inhibitors

(2015) David C. McKinney et al.   ACS Infectious Diseases

Molecular Basis of Selective Inhibition and Slow Reversibility of Avibactam against Class D Carbapenemases: A Structure-Guided Study of OXA-24 and OXA-48

(2014) Sushmita D. Lahiri et al.   ACS Chemical Biology

The Evolving Role of Chemical Synthesis in Antibacterial Drug Discovery

(2014) Peter M. Wright et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Renaissance of antibiotics against difficult infections: Focus on oritavancin and new ketolides and quinolones

(2014) Françoise Van Bambeke   ANNALS OF MEDICINE

Avibactam and Class C β-Lactamases: Mechanism of Inhibition, Conservation of the Binding Pocket, and Implications for Resistance

(2014) S. D. Lahiri et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Discovery of MK-7655, a β-lactamase inhibitor for combination with Primaxin®

(2014) Timothy A. Blizzard et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Merging Allosteric and Active Site Binding Motifs: De novo Generation of Target Selectivity and Potency via Natural-Product-Derived Fragments

(2014) Jan Lanz et al.   ChemMedChem

Oritavancin: First Global Approval

(2014) Anthony Markham   DRUGS

Siderophore Receptor-Mediated Uptake of Lactivicin Analogues in Gram-Negative Bacteria

(2014) Jeremy Starr et al.   JOURNAL OF MEDICINAL CHEMISTRY

Disruption of Allosteric Response as an Unprecedented Mechanism of Resistance to Antibiotics

(2014) Jennifer Fishovitz et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Thiopeptide Antibiotics: Retrospective and Recent Advances

(2014) Xavier Just-Baringo et al.   Marine Drugs

Combating Multidrug-Resistant Bacteria: Current Strategies for the Discovery of Novel Antibacterials

(2013) Kieron M. G. O'Connell et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Proliferation and significance of clinically relevant β-lactamases

(2013) Karen Bush   Annals of the New York Academy of Sciences

Insights into the Mode of Action of Novel Fluoroketolides, Potent Inhibitors of Bacterial Protein Synthesis

(2013) Marios G. Krokidis et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Structural Insight into Potent Broad-Spectrum Inhibition with Reversible Recyclization Mechanism: Avibactam in Complex with CTX-M-15 and Pseudomonas aeruginosa AmpC β-Lactamases

(2013) Sushmita D. Lahiri et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

In VitroandIn VivoAntibacterial Activities of Omadacycline, a Novel Aminomethylcycline

(2013) A. B. Macone et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Mechanism of Action of the Novel Aminomethylcycline Antibiotic Omadacycline

(2013) Michael P. Draper et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Strategic Targeting of Multiple Water-Mediated Interactions: A Concise and Rational Structure-Based Design Approach to Potent and Selective MMP-13 Inhibitors

(2013) Thomas Fischer et al.   ChemMedChem

Ceftolozane/Tazobactam: A Novel Cephalosporin/β-Lactamase Inhibitor Combination with Activity Against Multidrug-Resistant Gram-Negative Bacilli

(2013) George G. Zhanel et al.   DRUGS

Activity of biapenem (RPX2003) combined with the boronate  -lactamase inhibitor RPX7009 against carbapenem-resistant Enterobacteriaceae

(2013) D. M. Livermore et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Combined effects of the siderophore monosulfactam BAL30072 and carbapenems on multidrug-resistant Gram-negative bacilli

(2013) B. Hofer et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Ribosome-targeting antibiotics and mechanisms of bacterial resistance

(2013) Daniel N. Wilson   NATURE REVIEWS MICROBIOLOGY

Structural basis for potent inhibitory activity of the antibiotic tigecycline during protein synthesis

(2013) L. Jenner et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

How allosteric control of Staphylococcus aureus penicillin binding protein 2a enables methicillin resistance and physiological function

(2013) L. H. Otero et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Resistance to antibiotics targeted to the bacterial cell wall

(2013) I. Nikolaidis et al.   PROTEIN SCIENCE

Redesign of Glycopeptide Antibiotics: Back to the Future

(2012) Robert C. James et al.   ACS Chemical Biology

How Should We Think About the Ribosome?

(2012) Peter B. Moore   Annual Review of Biophysics

NXL104 Irreversibly Inhibits the β-Lactamase from Mycobacterium tuberculosis

(2012) Hua Xu et al.   BIOCHEMISTRY

Fragment-Based Approaches in Drug Discovery and Chemical Biology

(2012) Duncan E. Scott et al.   BIOCHEMISTRY

Selective Protein Synthesis by Ribosomes with a Drug-Obstructed Exit Tunnel

(2012) Krishna Kannan et al.   CELL

Boron Containing Compounds as Protease Inhibitors

(2012) Reem Smoum et al.   CHEMICAL REVIEWS

Adjuvant strategies for potentiation of antibiotics to overcome antimicrobial resistance

(2012) Michel Pieren et al.   CURRENT OPINION IN PHARMACOLOGY

Comparison of the next-generation aminoglycoside plazomicin to gentamicin, tobramycin and amikacin

(2012) George G Zhanel et al.   Expert Review of Anti-Infective Therapy

Characterization of methicillin-resistant Staphylococcus aureus displaying increased MICs of ceftaroline

(2012) R. E. Mendes et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Antibiotic Optimization and Chemical Structure Stabilization of Thiomuracin A

(2012) Matthew J. LaMarche et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of LFF571: An Investigational Agent for Clostridium difficile Infection

(2012) Matthew J. LaMarche et al.   JOURNAL OF MEDICINAL CHEMISTRY

Transcription factors: from enhancer binding to developmental control

(2012) François Spitz et al.   NATURE REVIEWS GENETICS

Structural basis for TetM-mediated tetracycline resistance

(2012) A. Donhofer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Avibactam is a covalent, reversible, non- -lactam  -lactamase inhibitor

(2012) D. E. Ehmann et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The oxazolidinones: past, present, and future

(2011) Karen Joy Shaw et al.   Annals of the New York Academy of Sciences

Low Fitness Cost of the Multidrug Resistance Genecfr

(2011) Jacqueline M. LaMarre et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Antimicrobial Activity of CXA-101, a Novel Cephalosporin Tested in Combination with Tazobactam against Enterobacteriaceae, Pseudomonas aeruginosa, and Bacteroides fragilis Strains Having Various Resistance Phenotypes

(2011) Helio S. Sader et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

4-Aminothiazolyl analogs of GE2270 A: Design, synthesis and evaluation of imidazole analogs

(2011) Matthew J. LaMarche et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and SAR of novel benzoxaboroles as a new class of β-lactamase inhibitors

(2011) Yi Xia et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Diazabicyclooctanes (DBOs): a potent new class of non-β-lactam β-lactamase inhibitors

(2011) Ken Coleman   CURRENT OPINION IN MICROBIOLOGY

Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent

(2011) Weon Bin Im et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

In vitro activity of BAL30072 against Burkholderia pseudomallei

(2011) Takehiko Mima et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

In vivo and in vitro activity of the siderophore monosulfactam BAL30072 against Acinetobacter baumannii

(2011) T. A. Russo et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Ceftaroline fosamil: a new broad-spectrum cephalosporin

(2011) J. B. Laudano   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

In vitro activity of tedizolid (TR-700) against linezolid-resistant staphylococci

(2011) I. Rodriguez-Avial et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Antibacterial Optimization of 4-Aminothiazolyl Analogues of the Natural Product GE2270 A: Identification of the Cycloalkylcarboxylic Acids

(2011) Matthew J. LaMarche et al.   JOURNAL OF MEDICINAL CHEMISTRY

Ethionamide Boosters: Synthesis, Biological Activity, and Structure−Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors

(2011) Marion Flipo et al.   JOURNAL OF MEDICINAL CHEMISTRY

4-Aminothiazolyl Analogues of GE2270 A: Antibacterial Lead Finding

(2011) Matthew J. LaMarche et al.   JOURNAL OF MEDICINAL CHEMISTRY

Activities of NXL104 Combinations with Ceftazidime and Aztreonam against Carbapenemase-ProducingEnterobacteriaceae

(2010) David M. Livermore et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Structure-Activity Relationships of Diverse Oxazolidinones for Linezolid-Resistant Staphylococcus aureus Strains Possessing the cfr Methyltransferase Gene or Ribosomal Mutations

(2010) J. B. Locke et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Molecular Characterization of Off-Target Activities of Telithromycin: a Potential Role for Nicotinic Acetylcholine Receptors

(2010) D. Bertrand et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Binding and Action of CEM-101, a New Fluoroketolide Antibiotic That Inhibits Protein Synthesis

(2010) B. Llano-Sotelo et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

In Vitro Properties of BAL30072, a Novel Siderophore Sulfactam with Activity against Multiresistant Gram-Negative Bacilli

(2010) M. G. P. Page et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Three Decades of  -Lactamase Inhibitors

(2010) S. M. Drawz et al.   CLINICAL MICROBIOLOGY REVIEWS

Combating evolution with intelligent design: the neoglycoside ACHN-490

(2010) Eliana S Armstrong et al.   CURRENT OPINION IN MICROBIOLOGY

Aminoglycoside modifying enzymes

(2010) Maria S. Ramirez et al.   DRUG RESISTANCE UPDATES

Discovery of novel antibacterials

(2010) J Richard Miller et al.   Expert Opinion on Drug Discovery

New aminoglycoside antibiotics

(2010) Paola Dozzo et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Origins and Evolution of Antibiotic Resistance

(2010) J. Davies et al.   MICROBIOLOGY AND MOLECULAR BIOLOGY REVIEWS

Structures of the Escherichia coli ribosome with antibiotics bound near the peptidyl transferase center explain spectra of drug action

(2010) J. A. Dunkle et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural basis for effectiveness of siderophore-conjugated monocarbams against clinically relevant strains of Pseudomonas aeruginosa

(2010) S. Han et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Ceftobiprole

(2009) George G Zhanel et al.   AMERICAN JOURNAL OF CLINICAL DERMATOLOGY

Activity of a New Antipseudomonal Cephalosporin, CXA-101 (FR264205), against Carbapenem-Resistant and Multidrug-Resistant Pseudomonas aeruginosa Clinical Strains

(2009) C. Juan et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

In Vitro Activity of NXL104 in Combination with  -Lactams against Klebsiella pneumoniae Isolates Producing KPC Carbapenemases

(2009) A. Endimiani et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

The tetracycline resistome

(2009) Maulik Thaker et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

The A–Z of bacterial translation inhibitors

(2009) Daniel N. Wilson   CRITICAL REVIEWS IN BIOCHEMISTRY AND MOLECULAR BIOLOGY

Ceftaroline

(2009) George G. Zhanel et al.   DRUGS

Activity of the siderophore monobactam BAL30072 against multiresistant non-fermenters

(2009) S. Mushtaq et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Ribosomally Synthesized Thiopeptide Antibiotics Targeting Elongation Factor Tu

(2009) Rowan P. Morris et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Synthetic EthR inhibitors boost antituberculous activity of ethionamide

(2009) Nicolas Willand et al.   NATURE MEDICINE

In Vitro Activities of the Rx-01 Oxazolidinones against Hospital and Community Pathogens

(2008) L. Lawrence et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

R -01, a New Family of Oxazolidinones That Overcome Ribosome-Based Linezolid Resistance

(2008) E. Skripkin et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

In Vitro Activity of TR-700, the Antibacterial Moiety of the Prodrug TR-701, against Linezolid-Resistant Strains

(2008) K. J. Shaw et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Transcriptional and Translational Control of the mlr Operon, Which Confers Resistance to Seven Classes of Protein Synthesis Inhibitors

(2008) L. K. Smith et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Design at the atomic level: Design of biaryloxazolidinones as potent orally active antibiotics

(2008) Jiacheng Zhou et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and SAR of novel parenteral anti-pseudomonal cephalosporins: Discovery of FR264205

(2008) Ayako Toda et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design at the atomic level: Generation of novel hybrid biaryloxazolidinones as promising new antibiotics

(2008) Jiacheng Zhou et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Macrolide myths

(2008) Alexander S Mankin   CURRENT OPINION IN MICROBIOLOGY

Telithromycin-associated hepatotoxicity: Clinical spectrum and causality assessment of 42 cases

(2008) Allen D. Brinker et al.   HEPATOLOGY

Restoration of Susceptibility of Methicillin-resistantStaphylococcus aureusto β-Lactam Antibiotics by Acidic pH

(2008) Sandrine Lemaire et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Crystal Structure of the Oxazolidinone Antibiotic Linezolid Bound to the 50S Ribosomal Subunit∥

(2008) Joseph A. Ippolito et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystal Structures of the Complexes between Vancomycin and Cell-Wall Precursor Analogs

(2008) Yasushi Nitanai et al.   JOURNAL OF MOLECULAR BIOLOGY

Translational Regulation via L11: Molecular Switches on the Ribosome Turned On and Off by Thiostrepton and Micrococcin

(2008) Joerg M. Harms et al.   MOLECULAR CELL

A structural understanding of the dynamic ribosome machine

(2008) Thomas A. Steitz   NATURE REVIEWS MOLECULAR CELL BIOLOGY

The oxazolidinone antibiotics perturb the ribosomal peptidyl-transferase center and effect tRNA positioning

(2008) D. N. Wilson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA