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2q5u

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[[Image:2q5u.gif|left|200px]]
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{{STRUCTURE_2q5u| PDB=2q5u | SCENE= }}
{{STRUCTURE_2q5u| PDB=2q5u | SCENE= }}
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'''Crystal structure of IQN17'''
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===Crystal structure of IQN17===
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==Overview==
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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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{{ABSTRACT_PUBMED_10520998}}
==About this Structure==
==About this Structure==
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[[Category: Envelope glycoprotein]]
[[Category: Envelope glycoprotein]]
[[Category: Viral protein/viral protein inhibitor]]
[[Category: Viral protein/viral protein inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:24:42 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 12:48:01 2008''

Revision as of 09:48, 27 July 2008

Image:2q5u.png

Template:STRUCTURE 2q5u

Crystal structure of IQN17

Template:ABSTRACT PUBMED 10520998

About this Structure

2Q5U is a Single protein structure. Full crystallographic information is available from OCA.

Reference

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 Jul 27 12:48:01 2008

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