2q5u: Difference between revisions
New page: left|200px<br /> <applet load="2q5u" size="450" color="white" frame="true" align="right" spinBox="true" caption="2q5u, resolution 1.50Å" /> '''Crystal structure o... |
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[[Image:2q5u.gif|left|200px]]<br /> | [[Image:2q5u.gif|left|200px]]<br /><applet load="2q5u" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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caption="2q5u, resolution 1.50Å" /> | caption="2q5u, resolution 1.50Å" /> | ||
'''Crystal structure of IQN17'''<br /> | '''Crystal structure of IQN17'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
2Q5U 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:// | 2Q5U is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/ ] with <scene name='pdbligand=CL:'>CL</scene> and <scene name='pdbligand=ACE:'>ACE</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q5U OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: viral protein/viral protein inhibitor]] | [[Category: viral protein/viral protein inhibitor]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 14:56:43 2008'' | ||
Revision as of 15:56, 23 January 2008
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Crystal structure of IQN17
OverviewOverview
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.
About this StructureAbout this Structure
2Q5U is a Single protein structure of sequence from [1] with and as ligands. Full crystallographic information is available from OCA.
ReferenceReference
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
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