Search Results - "Dale, Glenn"
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The Role of Neutrophil Elastase Inhibitors in Lung Diseases
Published in Chest (01-08-2017)“…In many respiratory diseases characterized by an intense inflammatory response, the balance between proteolytic enzymes (proteases, including elastases) and…”
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2
Murepavadin: a new antibiotic class in the pipeline
Published in Expert review of anti-infective therapy (03-04-2018)“…With the increase in multi-drug resistant P. aeruginosa, antimicrobials with a novel mechanism of action are needed that can target these infections. Areas…”
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3
Chimeric peptidomimetic antibiotics against Gram-negative bacteria
Published in Nature (London) (01-12-2019)“…There is an urgent need for new antibiotics against Gram-negative pathogens that are resistant to carbapenem and third-generation cephalosporins, against which…”
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Pharmacokinetics and Safety of Intravenous Murepavadin Infusion in Healthy Adult Subjects Administered Single and Multiple Ascending Doses
Published in Antimicrobial agents and chemotherapy (01-04-2018)“…Murepavadin is the first in class of the outer membrane protein-targeting antibiotics (OMPTA) and a pathogen-specific peptidomimetic antibacterial with a…”
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5
Protein epitope mimetic macrocycles as biopharmaceuticals
Published in Current opinion in chemical biology (01-06-2017)“…[Display omitted] •Medium-sized macrocycles can address novel disease-relevant targets.•Protein epitope mimetics (PEM) are mimics β-hairpin and α-helical…”
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Antimicrobial Activity of Murepavadin Tested against Clinical Isolates of Pseudomonas aeruginosa from the United States, Europe, and China
Published in Antimicrobial agents and chemotherapy (01-07-2018)“…Murepavadin (formerly POL7080), a 14-amino-acid cyclic peptide, and comparators were tested by the broth microdilution method against 1,219 isolates from 112…”
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Rifabutin for infusion (BV100) for the treatment of severe carbapenem-resistant Acinetobacter baumannii infections
Published in Drug discovery today (01-09-2021)“…•A unexpected activity of rifabutin (RBT) towards A. baumanni has been discovered.•RBT displays a potent activity towards A. baumannii in iron depleted…”
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Pharmacokinetics, Tolerability, and Safety of Murepavadin, a Novel Antipseudomonal Antibiotic, in Subjects with Mild, Moderate, or Severe Renal Function Impairment
Published in Antimicrobial agents and chemotherapy (01-09-2018)“…This open-label, nonrandomized, single-dose, phase 1 study evaluated the pharmacokinetics and safety of murepavadin, a novel peptide antibiotic for the…”
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Murepavadin activity tested against contemporary (2016-17) clinical isolates of XDR Pseudomonas aeruginosa
Published in Journal of antimicrobial chemotherapy (01-09-2018)“…Murepavadin (POL7080) represents the first member of a novel class of outer membrane protein-targeting antibiotics. Murepavadin acts by binding to LPS…”
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10
Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration
Published in European journal of medicinal chemistry (05-08-2022)“…Acinetobacter baumannii is a gram-negative bacterium causing severe hospital-acquired infections such as bloodstream infections or pneumonia. Moreover,…”
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In vitro activity of rifabutin against 293 contemporary carbapenem-resistant Acinetobacter baumannii clinical isolates and characterization of rifabutin mode of action and resistance mechanisms
Published in Journal of antimicrobial chemotherapy (01-12-2020)“…Abstract Background Rifabutin, an oral drug approved to treat Mycobacterium avium infections, demonstrated potent activity against Acinetobacter baumannii in…”
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12
First-in-human study of alpibectir (BVL-GSK098), a novel potent anti-TB drug
Published in Journal of antimicrobial chemotherapy (03-06-2024)“…The clinical candidate alpibectir augments the activity of, and overcomes resistance to, the anti-TB drug ethionamide in vitro and in vivo. A Phase 1,…”
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Susceptibility of Pseudomonas aeruginosa Recovered from Cystic Fibrosis Patients to Murepavadin and 13 Comparator Antibiotics
Published in Antimicrobial agents and chemotherapy (27-01-2020)“…The objective was to determine the antimicrobial susceptibility of isolates cultured from cystic fibrosis (CF) patients and explore associations between strain…”
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Antimicrobial activity of POL7306 tested against clinical isolates of Gram-negative bacteria collected worldwide
Published in Journal of antimicrobial chemotherapy (01-06-2020)“…POL7306 belongs to a new class of peptidomimetic outer-membrane-protein-targeting antibiotics with a novel mechanism of action. POL7306 is in development for…”
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15
Efficacy of the Novel Antibiotic POL7001 in Preclinical Models of Pseudomonas aeruginosa Pneumonia
Published in Antimicrobial agents and chemotherapy (01-08-2016)“…The clinical development of antibiotics with a new mode of action combined with efficient pulmonary drug delivery is a priority against untreatable Pseudomonas…”
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Structure of human Endothelin-converting Enzyme I Complexed with Phosphoramidon
Published in Journal of molecular biology (09-01-2009)“…Endothelin-converting enzyme I (ECE-1) is a mammalian type II integral membrane zinc-containing endopeptidase. ECE-1 catalyzes the final step in the…”
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A nutrient-limited screen unmasks rifabutin hyperactivity for extensively drug-resistant Acinetobacter baumannii
Published in Nature microbiology (01-09-2020)“…Industry screens of large chemical libraries have traditionally relied on rich media to ensure rapid bacterial growth in high-throughput testing. We used…”
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Mapping the active site of Escherichia coli malonyl-CoA-acyl carrier protein transacylase (FabD) by protein crystallography
Published in Acta crystallographica. Section D, Biological crystallography. (01-06-2006)“…Malonyl‐CoA–acyl carrier protein transacylase (FabD; EC 2.3.1.39) is a key enzyme in the fatty‐acid biosynthesis pathway of bacteria, catalyzing the transfer…”
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The protein as a variable in protein crystallization
Published in Journal of structural biology (01-04-2003)“…Strategies for growing protein crystals have for many years been essentially empirical, the protein, once purified to a certain homogeneity, being mixed with a…”
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Author Correction: Chimeric peptidomimetic antibiotics against Gram-negative bacteria
Published in Nature (London) (12-12-2019)“…An Amendment to this paper has been published and can be accessed via a link at the top of the paper…”
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