1qr8

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[[Image:1qr8.jpg|left|200px]]
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{{STRUCTURE_1qr8| PDB=1qr8 | SCENE= }}
{{STRUCTURE_1qr8| PDB=1qr8 | SCENE= }}
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'''INHIBITION OF HIV-1 INFECTIVITY BY THE GP41 CORE: ROLE OF A CONSERVED HYDROPHOBIC CAVITY IN MEMBRANE FUSION'''
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===INHIBITION OF HIV-1 INFECTIVITY BY THE GP41 CORE: ROLE OF A CONSERVED HYDROPHOBIC CAVITY IN MEMBRANE FUSION===
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==Overview==
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The gp41 envelope protein of human immunodeficiency virus type 1 (HIV-1) contains an alpha-helical core structure responsible for mediating membrane fusion during viral entry. Recent studies suggest that a conserved hydrophobic cavity in the coiled coil of this core plays a distinctive structural role in maintaining the fusogenic conformation of the gp41 molecule. Here we investigated the importance of this cavity in determining the structure and biological activity of the gp41 core by using the N34(L6)C28 model. The high-resolution crystal structures of N34(L6)C28 of two HIV-1 gp41 fusion-defective mutants reveal that each mutant sequence is accommodated in the six-helix bundle structure by forming the cavity with different sets of atoms. Remarkably, the mutant N34(L6)C28 cores are highly effective inhibitors of HIV-1 infection, with 5- to 16-fold greater activity than the wild-type molecule. The enhanced inhibitory activity by fusion-defective mutations correlates with local structural perturbations close to the cavity that destabilize the six-helix bundle. Taken together, these results indicate that the conserved hydrophobic coiled-coil cavity in the gp41 core is critical for HIV-1 entry and its inhibition and provides a potential antiviral drug target.
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(as it appears on PubMed at http://www.pubmed.gov), where 10482611 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10482611}}
==About this Structure==
==About this Structure==
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[[Category: Hiv-1 inhibition]]
[[Category: Hiv-1 inhibition]]
[[Category: Membrane fusion]]
[[Category: Membrane fusion]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 06:36:48 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 15:51:36 2008''

Revision as of 12:51, 28 July 2008

Image:1qr8.png

Template:STRUCTURE 1qr8

INHIBITION OF HIV-1 INFECTIVITY BY THE GP41 CORE: ROLE OF A CONSERVED HYDROPHOBIC CAVITY IN MEMBRANE FUSION

Template:ABSTRACT PUBMED 10482611

About this Structure

1QR8 is a Single protein structure of sequence from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.

Reference

Inhibition of human immunodeficiency virus type 1 infectivity by the gp41 core: role of a conserved hydrophobic cavity in membrane fusion., Ji H, Shu W, Burling FT, Jiang S, Lu M, J Virol. 1999 Oct;73(10):8578-86. PMID:10482611

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