1czq

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{{STRUCTURE_1czq| PDB=1czq | SCENE= }}
{{STRUCTURE_1czq| PDB=1czq | SCENE= }}
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'''CRYSTAL STRUCTURE OF THE D10-P1/IQN17 COMPLEX: A D-PEPTIDE INHIBITOR OF HIV-1 ENTRY BOUND TO THE GP41 COILED-COIL POCKET.'''
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===CRYSTAL STRUCTURE OF THE D10-P1/IQN17 COMPLEX: A D-PEPTIDE INHIBITOR OF HIV-1 ENTRY BOUND TO THE GP41 COILED-COIL POCKET.===
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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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(as it appears on PubMed at http://www.pubmed.gov), where 10520998 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10520998}}
==About this Structure==
==About this Structure==
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[[Category: Coiled coil]]
[[Category: Coiled coil]]
[[Category: Envelope glycoprotein]]
[[Category: Envelope glycoprotein]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 13:17:01 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 21:53:17 2008''

Revision as of 18:53, 30 June 2008

Image:1czq.png

Template:STRUCTURE 1czq

CRYSTAL STRUCTURE OF THE D10-P1/IQN17 COMPLEX: A D-PEPTIDE INHIBITOR OF HIV-1 ENTRY BOUND TO THE GP41 COILED-COIL POCKET.

Template:ABSTRACT PUBMED 10520998

About this Structure

1CZQ is a Single protein structure of sequence from Saccharomyces cerevisiae and human immunodeficiency virus. 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

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