3l35
From Proteopedia
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- | {{STRUCTURE_3l35| PDB=3l35 | SCENE= }} | ||
- | ===PIE12 D-peptide against HIV entry=== | ||
- | {{ABSTRACT_PUBMED_20719956}} | ||
- | == | + | ==PIE12 D-peptide against HIV entry== |
- | [[3l35]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3L35 OCA]. | + | <StructureSection load='3l35' size='340' side='right'caption='[[3l35]], [[Resolution|resolution]] 1.55Å' scene=''> |
+ | == Structural highlights == | ||
+ | <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 [https://proteopedia.org/fgij/fg.htm?mol=3L35 FirstGlance]. <br> | ||
+ | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.55Å</td></tr> | ||
+ | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3l35 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3l35 OCA], [https://pdbe.org/3l35 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3l35 RCSB], [https://www.ebi.ac.uk/pdbsum/3l35 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3l35 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> | |
- | <ref | + | |
- | [[Category: Eckert | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> |
- | [[Category: Hill | + | </div> |
- | [[Category: Kay | + | <div class="pdbe-citations 3l35" style="background-color:#fffaf0;"></div> |
- | [[Category: Lie | + | == References == |
- | [[Category: Paul | + | <references/> |
- | [[Category: Redman | + | __TOC__ |
- | [[Category: Reeves | + | </StructureSection> |
- | [[Category: Root | + | [[Category: Large Structures]] |
- | [[Category: Weinstock | + | [[Category: Eckert DM]] |
- | [[Category: Welch | + | [[Category: Hill CP]] |
- | [[Category: Whitby | + | [[Category: Kay MS]] |
- | + | [[Category: Lie YS]] | |
- | + | [[Category: Paul S]] | |
- | + | [[Category: Redman JS]] | |
+ | [[Category: Reeves JD]] | ||
+ | [[Category: Root MJ]] | ||
+ | [[Category: Weinstock MT]] | ||
+ | [[Category: Welch BD]] | ||
+ | [[Category: Whitby FG]] |
Current revision
PIE12 D-peptide against HIV entry
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Categories: Large Structures | Eckert DM | Hill CP | Kay MS | Lie YS | Paul S | Redman JS | Reeves JD | Root MJ | Weinstock MT | Welch BD | Whitby FG