2q5u

From Proteopedia

(Difference between revisions)

Revision as of 07:48, 9 March 2022

Crystal structure of IQN17

Structural highlights

2q5u is a 3 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
NonStd Res:
Related:	1czq, 2q3i
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[A3F986_9HIV1] The envelope glyprotein gp160 precursor down-modulates cell surface CD4 antigen by interacting with it in the endoplasmic reticulum and blocking its transport to the cell surface.[RuleBase:RU004292]

Publication Abstract from PubMed

The HIV-1 gp41 protein promotes viral entry by mediating the fusion of viral and cellular membranes. A prominent pocket on the surface of a central trimeric coiled coil within gp41 was previously identified as a potential target for drugs that inhibit HIV-1 entry. We designed a peptide, IQN17, which properly presents this pocket. Utilizing IQN17 and mirror-image phage display, we identified cyclic, D-peptide inhibitors of HIV-1 infection that share a sequence motif. A 1.5 A cocrystal structure of IQN17 in complex with a D-peptide, and NMR studies, show that conserved residues of these inhibitors make intimate contact with the gp41 pocket. Our studies validate the pocket per se as a target for drug development. IQN17 and these D-peptide inhibitors are likely to be useful for development and identification of a new class of orally bioavailable anti-HIV drugs.

Inhibiting HIV-1 entry: discovery of D-peptide inhibitors that target the gp41 coiled-coil pocket.,Eckert DM, Malashkevich VN, Hong LH, Carr PA, Kim PS Cell. 1999 Oct 1;99(1):103-15. PMID:10520998^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Eckert DM, Malashkevich VN, Hong LH, Carr PA, Kim PS. Inhibiting HIV-1 entry: discovery of D-peptide inhibitors that target the gp41 coiled-coil pocket. Cell. 1999 Oct 1;99(1):103-15. PMID:10520998

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 See Also
5 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2q5u"

@@ Line 3: / Line 3: @@
 <StructureSection load='2q5u' size='340' side='right'caption='[[2q5u]], [[Resolution|resolution]] 1.50&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[2q5u]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q5U OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=2Q5U FirstGlance]. <br>
+<table><tr><td colspan='2'>[[2q5u]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q5U OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2Q5U FirstGlance]. <br>
 </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</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></td></tr>
-<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1czq|1czq]], [[2q3i|2q3i]]</td></tr>
+<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1czq|1czq]], [[2q3i|2q3i]]</div></td></tr>
-<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=2q5u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2q5u OCA], [http://pdbe.org/2q5u PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2q5u RCSB], [http://www.ebi.ac.uk/pdbsum/2q5u PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2q5u ProSAT]</span></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=2q5u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2q5u OCA], [https://pdbe.org/2q5u PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2q5u RCSB], [https://www.ebi.ac.uk/pdbsum/2q5u PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2q5u ProSAT]</span></td></tr>
 </table>
 == Function ==
-[[http://www.uniprot.org/uniprot/A3F986_9HIV1 A3F986_9HIV1]] The envelope glyprotein gp160 precursor down-modulates cell surface CD4 antigen by interacting with it in the endoplasmic reticulum and blocking its transport to the cell surface.[RuleBase:RU004292]
+[[https://www.uniprot.org/uniprot/A3F986_9HIV1 A3F986_9HIV1]] The envelope glyprotein gp160 precursor down-modulates cell surface CD4 antigen by interacting with it in the endoplasmic reticulum and blocking its transport to the cell surface.[RuleBase:RU004292]
 <div style="background-color:#fffaf0;">
 == Publication Abstract from PubMed ==

2q5u

From Proteopedia

Revision as of 07:48, 9 March 2022

Crystal structure of IQN17

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

Contents

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