共查询到20条相似文献,搜索用时 0 毫秒
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Nicki Frederiksen Stavroula Louka Chirag Mudaliar Ilona Domraceva Agrita Kreicberga Osvalds Pugovics Dorota abicka Magdalena Tomczak Weronika Wygoda Fredrik Bjrkling Henrik Franzyk 《International journal of molecular sciences》2021,22(13)
PEGylation of antimicrobial peptides as a shielding tool that increases stability toward proteolytic degradation typically leads to concomitant loss of activity, whereas incorporation of ultrashort PEG-like amino acids (sPEGs) remains essentially unexplored. Here, modification of a peptide/β-peptoid hybrid with sPEGs was examined with respect to influence on hydrophobicity, antibacterial activity and effect on viability of mammalian cells for a set of 18 oligomers. Intriguingly, the degree of sPEG modification did not significantly affect hydrophobicity as measured by retention in reverse-phase HPLC. Antibacterial activity against both wild-type and drug-resistant strains of Escherichia coli and Acinetobacter baumannii (both Gram-negative pathogens) was retained or slightly improved (MICs in the range 2–16 µg/mL equal to 0.7–5.2 µM). All compounds in the series exhibited less than 10% hemolysis at 400 µg/mL. While the number of sPEG moieties appeared not to be clearly correlated with hemolytic activity, a trend toward slightly increased hemolytic activity was observed for analogues displaying the longest sPEGs. In contrast, within a subseries the viability of HepG2 liver cells was least affected by analogues displaying the longer sPEGs (with IC50 values of ~1280 µg/mL) as compared to most other analogues and the parent peptidomimetic (IC50 values in the range 330–800 µg/mL). 相似文献
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Front Cover: Alanine and Lysine Scans of the LL‐37‐Derived Peptide Fragment KR‐12 Reveal Key Residues for Antimicrobial Activity (ChemBioChem 9/2018) 下载免费PDF全文
Dr. Sunithi Gunasekera Taj Muhammad Dr. Adam A. Strömstedt Dr. K. Johan Rosengren Prof. Dr. Ulf Göransson 《Chembiochem : a European journal of chemical biology》2018,19(9):891-891
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Inside Cover: Synthesis of 3′‐Fluoro‐tRNA Analogues for Exploring Non‐ribosomal Peptide Synthesis in Bacteria (ChemBioChem 3/2015) 下载免费PDF全文
Dr. Laura Iannazzo Guillaume Laisné Dr. Matthieu Fonvielle Dr. Emmanuelle Braud Dr. Jean‐Philippe Herbeuval Dr. Michel Arthur Dr. Mélanie Etheve‐Quelquejeu 《Chembiochem : a European journal of chemical biology》2015,16(3):350-350
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Cover Picture: Detection of Human α‐L‐Fucosidases by a Quinone Methide‐Generating Probe: Enhanced Activities in Response to Helicobacter pylori Infection (ChemBioChem 11/2015) 下载免费PDF全文
Manjula Nandakumar Yu‐Ling Hsu Jason C.‐Y Lin Chun Lo Prof. Lee‐Chiang Lo Prof. Chun‐Hung Lin 《Chembiochem : a European journal of chemical biology》2015,16(11):1525-1525
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Sylvain Petit Yann Duroc Dr. Valéry Larue Dr. Carmela Giglione Dr. Carole Léon Dr. Coralie Soulama Dr. Alexis Denis Dr. Frédéric Dardel Prof. Thierry Meinnel Dr. Isabelle Artaud Dr. 《ChemMedChem》2009,4(2):133-133
The cover picture shows a “reverse” indole derivative in complex with Bacillus stearothermophilus peptide deformylase (PDF). This compound was selected from a structure–activity relationship study as a potent inhibitor of bacterial PDFs and shows antibacterial activity toward Bacillus subtilis as well as other pathogens such as Streptococcus pneumoniae and Staphylococcus aureus. For more details, see the Full Paper by I. Artaud et al. on p. 261 ff.
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Mieon Son Yuri Lee Heeyong Hwang Dr. Soonsil Hyun Prof. Jaehoon Yu 《ChemMedChem》2013,8(10):1573-1573