1t55: Difference between revisions
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==Antibiotic Activity and Structural Analysis of a Scorpion-derived Antimicrobial peptide IsCT and Its Analogs== | |||
<StructureSection load='1t55' size='340' side='right'caption='[[1t55]]' scene=''> | |||
| | == Structural highlights == | ||
| | <table><tr><td colspan='2'>[[1t55]] 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=1T55 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1T55 FirstGlance]. <br> | ||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR</td></tr> | |||
<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> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1t55 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1t55 OCA], [https://pdbe.org/1t55 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1t55 RCSB], [https://www.ebi.ac.uk/pdbsum/1t55 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1t55 ProSAT]</span></td></tr> | |||
</table> | |||
== Function == | |||
[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> | |||
<div style="background-color:#fffaf0;"> | |||
== | == Publication Abstract from PubMed == | ||
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. | 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. | ||
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> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
<div class="pdbe-citations 1t55" style="background-color:#fffaf0;"></div> | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Large Structures]] | |||
[[Category: Opisthacanthus madagascariensis]] | [[Category: Opisthacanthus madagascariensis]] | ||
[[Category: Hahm KS]] | |||
[[Category: Hahm | [[Category: Kim K]] | ||
[[Category: Kim | [[Category: Kim Y]] | ||
[[Category: Kim | [[Category: Lee K]] | ||
[[Category: Lee | [[Category: Lim SS]] | ||
[[Category: Lim | [[Category: Shin SY]] | ||
[[Category: Shin | |||
