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Encapsulation of OZ439 into Nanoparticles for Supersaturated Drug Release in Oral Malaria Therapy
10.1021/acsinfecdis.7b00278 2018-04-12 Malaria poses a major burden on human health and is becoming increasingly difficult to treat due to the development of antimalarial drug resistance. The resistance issue is further exacerbated by a lack of patient adherence to multi-day dosing regimens. This ... |
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Flavin Storage and Sequestration by Mycobacterium tuberculosis Dodecin
10.1021/acsinfecdis.7b00237 2018-04-09 Dodecins are small flavin binding proteins occurring in archaea and bacteria. They are remarkable for binding dimers of flavins with their functional relevant aromatic isoalloxazine rings deeply covered. Bacterial dodecins are widely spread and found in a lar... |
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Sputum Active Polymyxin Lipopeptides: Activity against Cystic Fibrosis Pseudomonas aeruginosa Isolates and Their Interactions with Sputum Biomolecules
10.1021/acsinfecdis.7b00238 2018-04-02 The mucoid biofilm mode of growth of Pseudomonas aeruginosa (P. aeruginosa) in the lungs of cystic fibrosis patients makes eradication of infections with antibiotic therapy very difficult. The lipopeptide antibiotics polymyxin B and colistin are currently the... |
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Potent 1,2,4-Triazino[5,6b]indole-3-thioether Inhibitors of the Kanamycin Resistance Enzyme Eis from Mycobacterium tuberculosis
10.1021/acsinfecdis.8b00074 2018-03-30 A common cause of resistance to kanamycin (KAN) in tuberculosis is overexpression of the enhanced intracellular survival (Eis) protein. Eis is an acetyltransferase that multiacetylates KAN and other aminoglycosides, rendering them unable to bind the bacterial... |
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Enhancing Antibody Serodiagnosis Using a Controlled Peptide Coimmobilization Strategy
10.1021/acsinfecdis.8b00014 2018-03-29 Antigen immunoreactivity is often determined by surface regions defined by the 3D juxtapositions of amino acids stretches that are not continuous in the linear sequence. As such, mimicking an antigen immunoreactivity by means of putative linear peptide epitop... |
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Antibacterial Drug Discovery: Some Assembly Required
10.1021/acsinfecdis.8b00027 2018-03-29 Our limited understanding of the molecular basis for compound entry into and efflux out of Gram-negative bacteria is now recognized as a key bottleneck for the rational discovery of novel antibacterial compounds. Traditional, large-scale biochemical or target... |
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Biogenic and Biomimetic Carriers as Versatile Transporters To Treat Infections
10.1021/acsinfecdis.8b00030 2018-03-29 Biogenic and biomimetic therapeutics are a relatively new class of systems that are of physiological origin and/or take advantage of natural pathways or aim at mimicking these to improve selective interaction with target tissue. The number of biogenic and bio... |
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Copper Influences the Antibacterial Outcomes of a β-Lactamase-Activated Prochelator against Drug-Resistant Bacteria
10.1021/acsinfecdis.8b00037 2018-03-26 The unabated rise in bacterial resistance to conventional antibiotics, coupled with collateral damage to normal flora incurred by overuse of broad-spectrum antibiotics, necessitates the development of new antimicrobials targeted against pathogenic organisms. ... |
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2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure–Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization
10.1021/acsinfecdis.7b00275 2018-03-26 Mycobacterium tuberculosis (MTb) possesses two nonproton pumping type II NADH dehydrogenase (NDH-2) enzymes which are predicted to be jointly essential for respiratory metabolism. Furthermore, the structure of a closely related bacterial NDH-2 has been report... |
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Doxycycline Prophylaxis for Bacterial Sexually Transmitted Infections: Promises and Perils
10.1021/acsinfecdis.8b00043 2018-03-23 Despite their high global incidence, sexually transmitted infections (STIs) remain a neglected area of research. Increased rates of STIs have been reported in particular among men who have sex with men (MSM) probably because of the advances in the treatment a... |