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31.
Peptoid Efficacy against Polymicrobial Biofilms Determined by Using Propidium Monoazide‐Modified Quantitative PCR 下载免费PDF全文
Dr. Yu Luo Hannah L. Bolt Dr. Gabriela A. Eggimann Prof. Dr. Danny F. McAuley Dr. Ronan McMullan Dr. Tanya Curran Dr. Mei Zhou Professor Colin A. B. Jahoda Dr. Steven L. Cobb Dr. Fionnuala T. Lundy 《Chembiochem : a European journal of chemical biology》2017,18(1):111-118
Biofilms containing Candida albicans are responsible for a wide variety of clinical infections. The protective effects of the biofilm matrix, the low metabolic activity of microorganisms within a biofilm and their high mutation rate, significantly enhance the resistance of biofilms to conventional antimicrobial treatments. Peptoids are peptide‐mimics that share many features of host defence antimicrobial peptides but have increased resistance to proteases and therefore have better stability in vivo. The activity of a library of peptoids was tested against monospecies and polymicrobial bacterial/fungal biofilms. Selected peptoids showed significant bactericidal and fungicidal activity against the polymicrobial biofilms. This coupled with low cytotoxicity suggests that peptoids could offer a new option for the treatment of clinically relevant polymicrobial infections. 相似文献
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Enhancement of the oxygen gas barrier properties of polyethylene terephthalate (PET), used in the packaging industry, is the main objective here. For this purpose, nanocomposites of PET containing graphite nanoplatelets (GNPs) were prepared by melt compounding. The effects of the nanocomposites' structural morphology on oxygen gas permeability were analyzed using a range of thermal, microscopic, and mechanical characterization techniques. The investigated nanocomposite films exhibited GNP exfoliated morphology and good mixing with PET, as well as uniform dispersion within the polymer. All nanocomposite films were shown to possess superior oxygen barrier properties and improved thermal and dimensional stability compared with the plain PET films. In the best case, for 1.5 wt % GNP, the oxygen permeation was reduced by more than 99%. The improved barrier properties are attributed to the direct effect of the GNPs and to their induced increase of degree of crystallinity. © 2012 Wiley Periodicals, Inc. J. Appl. Polym. Sci., 2013 相似文献
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Hannah E. Rockwell Fei Gao Emily Y. Chen Justice McDaniel Rangaprasad Sarangarajan Niven R. Narain Michael A. Kiebish 《Lipids》2016,51(7):875-886
The development of enabling mass spectrometry platforms for the quantification of diverse lipid species in human urine is of paramount importance for understanding metabolic homeostasis in normal and pathophysiological conditions. Urine represents a non‐invasive biofluid that can capture distinct differences in an individual's physiological status. However, currently there is a lack of quantitative workflows to engage in high throughput lipidomic analysis. This study describes the development of a MS/MSALL shotgun lipidomic workflow and a micro liquid chromatography–high resolution tandem mass spectrometry (LC–MS/MS) workflow for urine structural and mediator lipid analysis, respectively. This workflow was deployed to understand biofluid sample handling and collection, extraction efficiency, and natural human variation over time. Utilization of 0.5 mL of urine for structural lipidomic analysis resulted in reproducible quantification of more than 600 lipid molecular species from over 20 lipid classes. Analysis of 1 mL of urine routinely quantified in excess of 55 mediator lipid metabolites comprised of octadecanoids, eicosanoids, and docosanoids generated by lipoxygenase, cyclooxygenase, and cytochrome P450 activities. In summary, the high‐throughput functional lipidomics workflow described in this study demonstrates an impressive robustness and reproducibility that can be utilized for population health and precision medicine applications. 相似文献
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Dr. Armin Welker Dr. Christian Kersten Dr. Christin Müller Dr. Ramakanth Madhugiri Collin Zimmer Patrick Müller Robert Zimmermann Stefan Hammerschmidt Hannah Maus Prof. John Ziebuhr Prof. Christoph Sotriffer Prof. Tanja Schirmeister 《ChemMedChem》2021,16(2):340-354
Inhibition of coronavirus (CoV)-encoded papain-like cysteine proteases (PLpro) represents an attractive strategy to treat infections by these important human pathogens. Herein we report on structure-activity relationships (SAR) of the noncovalent active-site directed inhibitor (R)-5-amino-2-methyl-N-(1-(naphthalen-1-yl)ethyl) benzamide ( 2 b ), which is known to bind into the S3 and S4 pockets of the SARS-CoV PLpro. Moreover, we report the discovery of isoindolines as a new class of potent PLpro inhibitors. The studies also provide a deeper understanding of the binding modes of this inhibitor class. Importantly, the inhibitors were also confirmed to inhibit SARS-CoV-2 replication in cell culture suggesting that, due to the high structural similarities of the target proteases, inhibitors identified against SARS-CoV PLpro are valuable starting points for the development of new pan-coronaviral inhibitors. 相似文献
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Manibarathi Vaithiyanathan Hannah C. Hymel Nora Safa Olivia M. Sanchez Jacob H. Pettigrew Cole S. Kirkpatrick Ted J. Gauthier Adam T. Melvin 《American Institute of Chemical Engineers》2021,67(1):e17087
Most cell penetrating peptides (CPPs) are unstructured and susceptible to proteolytic degradation. One alternative is to incorporate D-chirality amino acids into unstructured CPPs to allow for enhanced uptake and intracellular stability. This work investigates CPP internalization using a series of time, concentration, temperature, and energy dependent studies, resulting in a three-fold increase in uptake and 50-fold increase in stability of D-chirality peptides over L-chirality counterparts. CPP internalization occurred via a combination of direct penetration and endocytosis, with a percentage of internalized CPP expelling from cells in a time-dependent manner. Mechanistic studies identified that cells exported the intact internalized D-chirality CPPs via an exocytosis independent pathway, analogous to a direct penetration method out of the cells. These findings highlight the potential of a D-chirality CPP as bio-vector in therapeutic and biosensing applications, but also identify a new expulsion method suggesting a relationship between uptake kinetics, intracellular stability, and export kinetics. 相似文献
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Zhaoping Li Hannah Karp Alona Zerlin Tsz Ying Amy Lee Catherine Carpenter David Heber 《Nutrition journal》2010,9(1):44