Source:http://linkedlifedata.com/resource/pubmed/id/21308877
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
2011-2-10
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pubmed:abstractText |
Gramicidin S (GS) is a cyclo-decapeptide antibiotic isolated from Bacillus brevis. The structural studies have shown that GS forms a two-stranded antiparallel ?-sheet imposed by two II' ?-turns. Despite its wide Gram+ and Gram- antimicrobial spectrum, GS is useless in therapy because of its high hemotoxicity in humans. It was found, however, that the analogues of GS-14 (GS with 14 amino acid residues) attained a better antimicrobial selectivity when their amphipatic moments were perturbed. In this study, we report effects of similar perturbations imposed on GS cyclo-decapeptide analogues. Having solved their structures by NMR/molecular dynamics and having tested their activities/selectivities, we have concluded that the idea of perturbation of the amphipatic moment does not work for GS-10_0 analogues. An innovative approach to the synthesis of head-to-tail cyclopeptides was used.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
1099-1387
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pubmed:author | |
pubmed:copyrightInfo |
Copyright © 2010 European Peptide Society and John Wiley & Sons, Ltd.
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pubmed:issnType |
Electronic
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
211-7
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pubmed:meshHeading |
pubmed-meshheading:21308877-Amino Acid Sequence,
pubmed-meshheading:21308877-Anti-Bacterial Agents,
pubmed-meshheading:21308877-Cells, Cultured,
pubmed-meshheading:21308877-Gramicidin,
pubmed-meshheading:21308877-Hemolysis,
pubmed-meshheading:21308877-Humans,
pubmed-meshheading:21308877-Magnetic Resonance Spectroscopy,
pubmed-meshheading:21308877-Microbial Sensitivity Tests,
pubmed-meshheading:21308877-Molecular Sequence Data,
pubmed-meshheading:21308877-Structure-Activity Relationship
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pubmed:year |
2011
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pubmed:articleTitle |
Synthesis, biological activity and solution structure of new analogues of the antimicrobial Gramicidin S.
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pubmed:affiliation |
University of Gda?sk, Faculty of Chemistry, Sobieskiego 18, Gda?sk, 80-952, Poland. kamysz@chem.univ.gda.pl
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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