3l35

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{{STRUCTURE_3l35| PDB=3l35 | SCENE= }}
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==PIE12 D-peptide against HIV entry==
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===PIE12 D-peptide against HIV entry===
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<StructureSection load='3l35' size='340' side='right' caption='[[3l35]], [[Resolution|resolution]] 1.55&Aring;' scene=''>
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{{ABSTRACT_PUBMED_20719956}}
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3l35]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3L35 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3L35 FirstGlance]. <br>
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</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=DAS:D-ASPARTIC+ACID'>DAS</scene>, <scene name='pdbligand=DCY:D-CYSTEINE'>DCY</scene>, <scene name='pdbligand=DGL:D-GLUTAMIC+ACID'>DGL</scene>, <scene name='pdbligand=DGN:D-GLUTAMINE'>DGN</scene>, <scene name='pdbligand=DHI:D-HISTIDINE'>DHI</scene>, <scene name='pdbligand=DLE:D-LEUCINE'>DLE</scene>, <scene name='pdbligand=DLY:D-LYSINE'>DLY</scene>, <scene name='pdbligand=DPR:D-PROLINE'>DPR</scene>, <scene name='pdbligand=DTR:D-TRYPTOPHAN'>DTR</scene>, <scene name='pdbligand=DTY:D-TYROSINE'>DTY</scene>, <scene name='pdbligand=NH2:AMINO+GROUP'>NH2</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2r5d|2r5d]], [[3l36|3l36]]</td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3l35 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3l35 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3l35 RCSB], [http://www.ebi.ac.uk/pdbsum/3l35 PDBsum]</span></td></tr>
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</table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The HIV gp41 N-trimer pocket region is an ideal viral target because it is extracellular, highly conserved, and essential for viral entry. Here, we report on the design of a pocket-specific D-peptide, PIE12-trimer, that is extraordinarily elusive to resistance and characterize its inhibitory and structural properties. D-peptides (peptides composed of D-amino acids) are promising therapeutic agents due to their insensitivity to protease degradation. PIE12-trimer was designed using structure-guided mirror-image phage display and linker optimization and is the first D-peptide HIV entry inhibitor with the breadth and potency required for clinical use. PIE12-trimer has an ultrahigh affinity for the gp41 pocket, providing it with a reserve of binding energy (resistance capacitor) that yields a dramatically improved resistance profile compared to those of other fusion inhibitors. These results demonstrate that the gp41 pocket is an ideal drug target and establish PIE12-trimer as a leading anti-HIV antiviral candidate.
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==About this Structure==
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Design of a potent D-peptide HIV-1 entry inhibitor with a strong barrier to resistance.,Welch BD, Francis JN, Redman JS, Paul S, Weinstock MT, Reeves JD, Lie YS, Whitby FG, Eckert DM, Hill CP, Root MJ, Kay MS J Virol. 2010 Nov;84(21):11235-44. Epub 2010 Aug 18. PMID:20719956<ref>PMID:20719956</ref>
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[[3l35]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3L35 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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<ref group="xtra">PMID:020719956</ref><references group="xtra"/><references/>
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</div>
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[[Category: Eckert, D M.]]
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== References ==
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[[Category: Hill, C P.]]
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<references/>
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[[Category: Kay, M S.]]
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__TOC__
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[[Category: Lie, Y S.]]
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</StructureSection>
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[[Category: Paul, S.]]
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[[Category: Eckert, D M]]
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[[Category: Redman, J S.]]
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[[Category: Hill, C P]]
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[[Category: Reeves, J D.]]
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[[Category: Kay, M S]]
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[[Category: Root, M J.]]
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[[Category: Lie, Y S]]
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[[Category: Weinstock, M T.]]
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[[Category: Paul, S]]
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[[Category: Welch, B D.]]
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[[Category: Redman, J S]]
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[[Category: Whitby, F G.]]
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[[Category: Reeves, J D]]
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[[Category: Root, M J]]
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[[Category: Weinstock, M T]]
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[[Category: Welch, B D]]
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[[Category: Whitby, F G]]
[[Category: Coiled-coil]]
[[Category: Coiled-coil]]
[[Category: D-peptide inhibitor]]
[[Category: D-peptide inhibitor]]
[[Category: De novo protein]]
[[Category: De novo protein]]

Revision as of 15:13, 18 December 2014

PIE12 D-peptide against HIV entry

3l35, resolution 1.55Å

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