2q5u: Difference between revisions
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'''Crystal structure of IQN17''' | '''Crystal structure of IQN17''' | ||
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==About this Structure== | ==About this Structure== | ||
2Q5U is a [[Single protein]] structure | 2Q5U is a [[Single protein]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q5U OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Kim, P S.]] | [[Category: Kim, P S.]] | ||
[[Category: Malashkevich, V N.]] | [[Category: Malashkevich, V N.]] | ||
[[Category: | [[Category: Coiled coil]] | ||
[[Category: | [[Category: Envelope glycoprotein]] | ||
[[Category: | [[Category: Viral protein/viral protein inhibitor]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:24:42 2008'' | |||
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Revision as of 14:24, 4 May 2008
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. 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 Page seeded by OCA on Sun May 4 14:24:42 2008