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3l36
From Proteopedia
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| - | {{Seed}} | ||
| - | [[Image:3l36.jpg|left|200px]] | ||
| - | < | + | ==PIE12 D-peptide against HIV entry== |
| - | + | <StructureSection load='3l36' size='340' side='right'caption='[[3l36]], [[Resolution|resolution]] 1.45Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[3l36]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3L36 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3L36 FirstGlance]. <br> | |
| - | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CXS:3-CYCLOHEXYL-1-PROPYLSULFONIC+ACID'>CXS</scene></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> |
| - | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[2r5d|2r5d]], [[3l34|3l34]]</div></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=3l36 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3l36 OCA], [https://pdbe.org/3l36 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3l36 RCSB], [https://www.ebi.ac.uk/pdbsum/3l36 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3l36 ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | 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. | ||
| - | + | 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> | |
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 3l36" style="background-color:#fffaf0;"></div> | ||
| - | + | ==See Also== | |
| - | + | *[[Gp41 3D Structures|Gp41 3D Structures]] | |
| - | + | == References == | |
| - | + | <references/> | |
| - | + | __TOC__ | |
| - | + | </StructureSection> | |
| - | == | + | [[Category: Large Structures]] |
| - | + | [[Category: Eckert, D M]] | |
| - | + | [[Category: Hill, C P]] | |
| - | == | + | [[Category: Kay, M S]] |
| - | < | + | [[Category: Lie, Y S]] |
| - | [[Category: Eckert, D M | + | [[Category: Paul, S]] |
| - | [[Category: Hill, C P | + | [[Category: Redman, J S]] |
| - | [[Category: Kay, M S | + | [[Category: Reeves, J D]] |
| - | [[Category: Lie, Y S | + | [[Category: Root, M J]] |
| - | [[Category: Paul, S | + | [[Category: Weinstock, M T]] |
| - | [[Category: Redman, J S | + | [[Category: Welch, B D]] |
| - | [[Category: Reeves, J D | + | [[Category: Whitby, F G]] |
| - | [[Category: Root, M J | + | |
| - | [[Category: Weinstock, M T | + | |
| - | [[Category: Welch, B D | + | |
| - | [[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]] | ||
| - | |||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Nov 3 11:09:20 2010'' | ||
Current revision
PIE12 D-peptide against HIV entry
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