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6p9n
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==CRYSTAL STRUCTURE OF HIV-1 LM/HT CLADE A/E CRF01 GP120 CORE IN COMPLEX WITH (S)-MCG-IV-210.== | |
| + | <StructureSection load='6p9n' size='340' side='right'caption='[[6p9n]], [[Resolution|resolution]] 2.65Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[6p9n]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6P9N OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6P9N FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EPE:4-(2-HYDROXYETHYL)-1-PIPERAZINE+ETHANESULFONIC+ACID'>EPE</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=O51:(3S)-N~1~-(2-aminoethyl)-N~3~-(4-chloro-3-fluorophenyl)piperidine-1,3-dicarboxamide'>O51</scene></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=6p9n FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6p9n OCA], [http://pdbe.org/6p9n PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6p9n RCSB], [http://www.ebi.ac.uk/pdbsum/6p9n PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6p9n ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The HIV-1 envelope glycoprotein (Env) trimer mediates virus entry into cells. The "closed" conformation of Env is resistant to non-neutralizing antibodies (nnAbs). These antibodies mostly recognize occluded epitopes that can be exposed upon binding of CD4 or small-molecule CD4 mimetics (CD4mc). Here, we describe a new family of small molecules that expose Env to nnAbs and sensitize infected cells to antibody-dependent cellular cytotoxicity (ADCC). These compounds have limited capacity to inhibit virus infection directly, but are able to sensitize viral particles to neutralization by otherwise non-neutralizing antibodies. Structural analysis shows that some analogs of this family of CD4mc engage the gp120 Phe43 cavity by contacting the highly-conserved D368 residue, making them attractive scaffolds for drug development.IMPORTANCE HIV-1 has evolved multiple strategies to avoid humoral responses. One efficient mechanism is to keep its envelope glycoproteins (Env) in its "closed" conformation. Here we report on a new family of small molecules able to "open-up" Env, thus exposing vulnerable epitopes. This new family of molecules bind in the Phe43 cavity and contact the highly-conserved D368 residue. The structural and biological attributes of this family of molecules make them good candidates for drug development. | ||
| - | + | A new family of small-molecule CD4-mimetic compounds contact the highly conserved aspartic acid 368 of HIV-1 gp120 and mediates ADCC.,Ding S, Grenier MC, Tolbert WD, Vezina D, Sherburn R, Richard J, Prevost J, Chapleau JP, Gendron-Lepage G, Medjahed H, Abrams C, Sodroski J, Pazgier M, Smith AB 3rd, Finzi A J Virol. 2019 Sep 25. pii: JVI.01325-19. doi: 10.1128/JVI.01325-19. PMID:31554684<ref>PMID:31554684</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| + | <div class="pdbe-citations 6p9n" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Large Structures]] | ||
[[Category: Pazgier, M]] | [[Category: Pazgier, M]] | ||
| - | [[Category: Tolbert, W.D]] | ||
[[Category: Sherburn, R]] | [[Category: Sherburn, R]] | ||
| + | [[Category: Tolbert, W D]] | ||
| + | [[Category: Clade a/e cf01]] | ||
| + | [[Category: Hiv-1 gp120]] | ||
| + | [[Category: Immune system]] | ||
| + | [[Category: Viral protein]] | ||
Revision as of 06:57, 23 October 2019
CRYSTAL STRUCTURE OF HIV-1 LM/HT CLADE A/E CRF01 GP120 CORE IN COMPLEX WITH (S)-MCG-IV-210.
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