Source:http://linkedlifedata.com/resource/pubmed/id/15369808
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2004-9-16
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pubmed:abstractText |
IsCT is a non-cell-selective antimicrobial peptide isolated from the scorpion Opisthacanthus madagascariensis that has potent cytolytic activity against both mammalian and bacterial cells. To investigate the structure-activity relationships of IsCT and to design novel peptide antibiotics with bacterial cell selectivity, we synthesized several analogs of IsCT and determined their three-dimensional structures in solution by 2D-NMR spectroscopy. IsCT has a linear alpha-helical structure from Gly3 to Phe13, and [K7]-IsCT has a linear alpha-helical structure from Leu2 to Phe13. [K7, P8, K11]-IsCT, which has a bend in its middle region, exhibited the highest antibacterial activity without hemolytic activity, suggesting that its proline-induced bend is an important determinant of this selectivity. Tryptophan fluorescence showed that the high selectivity of [K7, P8, K11]-IsCT toward bacterial cells is closely correlated with its highly selective interaction with negatively charged phospholipids. Its potent activity against antibiotic-resistant bacteria suggests that [K7, P8, K11]-IsCT may serve as a promising lead candidate in the development of new peptide antibiotics.
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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 |
Oct
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pubmed:issn |
0006-291X
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pubmed:author | |
pubmed:copyrightInfo |
Copyright 2004 Elsevier Inc.
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
323
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
712-9
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15369808-Amino Acid Sequence,
pubmed-meshheading:15369808-Amino Acid Substitution,
pubmed-meshheading:15369808-Animals,
pubmed-meshheading:15369808-Anti-Bacterial Agents,
pubmed-meshheading:15369808-Bacteria,
pubmed-meshheading:15369808-Computer Simulation,
pubmed-meshheading:15369808-Dose-Response Relationship, Drug,
pubmed-meshheading:15369808-Hemolysis,
pubmed-meshheading:15369808-Humans,
pubmed-meshheading:15369808-Models, Molecular,
pubmed-meshheading:15369808-Molecular Sequence Data,
pubmed-meshheading:15369808-Scorpion Venoms,
pubmed-meshheading:15369808-Structure-Activity Relationship
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pubmed:year |
2004
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pubmed:articleTitle |
Antibiotic activity and structural analysis of the scorpion-derived antimicrobial peptide IsCT and its analogs.
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pubmed:affiliation |
Department of Chemistry and Bio/Molecular Informatics Center, Konkuk University, Seoul 143-701, Republic of Korea.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't,
Evaluation Studies
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