1t54

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(New page: 200px<br /><applet load="1t54" size="450" color="white" frame="true" align="right" spinBox="true" caption="1t54" /> '''Antibiotic Activity and Structural Analysis ...)
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'''Antibiotic Activity and Structural Analysis of a Scorpion-derived Antimicrobial peptide IsCT and Its Analogs'''<br />
 
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==Overview==
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==Antibiotic Activity and Structural Analysis of a Scorpion-derived Antimicrobial peptide IsCT and Its Analogs==
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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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<StructureSection load='1t54' size='340' side='right'caption='[[1t54]]' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[1t54]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Opisthacanthus_madagascariensis Opisthacanthus madagascariensis]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1T54 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1T54 FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR, 20 models</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NH2:AMINO+GROUP'>NH2</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1t54 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1t54 OCA], [https://pdbe.org/1t54 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1t54 RCSB], [https://www.ebi.ac.uk/pdbsum/1t54 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1t54 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/NDB41_OPIMA NDB41_OPIMA] Shows weak hemolytic activity and antibacterial activity against both Gram-positive and Gram-negative bacteria probably by forming pores in the cell membrane. IsCT adopts an amphipathic alpha-helical structure.<ref>PMID:11520071</ref> Shows neither hemolytic, nor antibacterial activities, probably because it cannot adopt amphipathic alpha-helical structure.<ref>PMID:12054688</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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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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==About this Structure==
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Antibiotic activity and structural analysis of the scorpion-derived antimicrobial peptide IsCT and its analogs.,Lee K, Shin SY, Kim K, Lim SS, Hahm KS, Kim Y Biochem Biophys Res Commun. 2004 Oct 15;323(2):712-9. PMID:15369808<ref>PMID:15369808</ref>
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1T54 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Opisthacanthus_madagascariensis Opisthacanthus madagascariensis] with NH2 as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1T54 OCA].
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==Reference==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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Antibiotic activity and structural analysis of the scorpion-derived antimicrobial peptide IsCT and its analogs., Lee K, Shin SY, Kim K, Lim SS, Hahm KS, Kim Y, Biochem Biophys Res Commun. 2004 Oct 15;323(2):712-9. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15369808 15369808]
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</div>
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<div class="pdbe-citations 1t54" style="background-color:#fffaf0;"></div>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Large Structures]]
[[Category: Opisthacanthus madagascariensis]]
[[Category: Opisthacanthus madagascariensis]]
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[[Category: Single protein]]
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[[Category: Hahm KS]]
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[[Category: Hahm, K.S.]]
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[[Category: Kim K]]
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[[Category: Kim, K.]]
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[[Category: Kim Y]]
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[[Category: Kim, Y.]]
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[[Category: Lee K]]
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[[Category: Lee, K.]]
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[[Category: Lim SS]]
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[[Category: Lim, S.S.]]
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[[Category: Shin SY]]
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[[Category: Shin, S.Y.]]
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[[Category: NH2]]
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[[Category: coil-helix]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Wed Nov 21 03:00:02 2007''
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Antibiotic Activity and Structural Analysis of a Scorpion-derived Antimicrobial peptide IsCT and Its Analogs

PDB ID 1t54

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