2q7c

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(New page: 200px<br /> <applet load="2q7c" size="450" color="white" frame="true" align="right" spinBox="true" caption="2q7c, resolution 2.00&Aring;" /> '''Crystal structure o...)
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[[Image:2q7c.gif|left|200px]]<br />
 
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<applet load="2q7c" size="450" color="white" frame="true" align="right" spinBox="true"
 
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caption="2q7c, resolution 2.00&Aring;" />
 
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'''Crystal structure of IQN17'''<br />
 
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==Overview==
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==Crystal structure of IQN17==
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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.
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<StructureSection load='2q7c' size='340' side='right'caption='[[2q7c]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2q7c]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q7C OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2Q7C FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2&#8491;</td></tr>
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<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=CL:CHLORIDE+ION'>CL</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2q7c FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2q7c OCA], [https://pdbe.org/2q7c PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2q7c RCSB], [https://www.ebi.ac.uk/pdbsum/2q7c PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2q7c ProSAT]</span></td></tr>
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</table>
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== Function ==
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[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]
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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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.
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==About this Structure==
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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<ref>PMID:10520998</ref>
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2Q7C is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/ ] with CL and ACE as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2Q7C OCA].
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==Reference==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=10520998 10520998]
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</div>
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[[Category: Single protein]]
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<div class="pdbe-citations 2q7c" style="background-color:#fffaf0;"></div>
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[[Category: Eckert, D.M.]]
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[[Category: Hong, L.H.]]
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[[Category: Kim, P.S.]]
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[[Category: Malashkevich, V.N.]]
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[[Category: ACE]]
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[[Category: CL]]
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[[Category: coiled coil]]
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[[Category: envelope glycoprotein]]
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[[Category: viral protein/viral protein inhibitor]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Thu Nov 8 14:57:24 2007''
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==See Also==
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*[[Gcn4 3D Structures|Gcn4 3D Structures]]
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*[[Gnc4 3D Structures|Gnc4 3D Structures]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Human immunodeficiency virus 1]]
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[[Category: Large Structures]]
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[[Category: Eckert DM]]
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[[Category: Hong LH]]
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[[Category: Kim PS]]
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[[Category: Malashkevich VN]]

Current revision

Crystal structure of IQN17

PDB ID 2q7c

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