3l35: Difference between revisions
From Proteopedia
Jump to navigationJump to search
m Protected "3l35" [edit=sysop:move=sysop] |
No edit summary |
||
| Line 1: | Line 1: | ||
==PIE12 D-peptide against HIV entry== | |||
===PIE12 D-peptide | <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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3L35 FirstGlance]. <br> | |||
</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">[[2r5d|2r5d]], [[3l36|3l36]]</td></tr> | |||
<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> | |||
</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> | |||
[[Category: Eckert, D M | == References == | ||
[[Category: Hill, C P | <references/> | ||
[[Category: Kay, M S | __TOC__ | ||
[[Category: Lie, Y S | </StructureSection> | ||
[[Category: Paul, S | [[Category: Eckert, D M]] | ||
[[Category: Redman, J S | [[Category: Hill, C P]] | ||
[[Category: Reeves, J D | [[Category: Kay, M S]] | ||
[[Category: Root, M J | [[Category: Lie, Y S]] | ||
[[Category: Weinstock, M T | [[Category: Paul, S]] | ||
[[Category: Welch, B D | [[Category: Redman, J S]] | ||
[[Category: Whitby, F G | [[Category: Reeves, J D]] | ||
[[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]] | ||
Revision as of 15:13, 18 December 2014
PIE12 D-peptide against HIV entry
| ||||||||||||
