1qr9
From Proteopedia
(New page: 200px<br /> <applet load="1qr9" size="450" color="white" frame="true" align="right" spinBox="true" caption="1qr9, resolution 1.60Å" /> '''INHIBITION OF HIV-1...) |
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caption="1qr9, resolution 1.60Å" /> | caption="1qr9, resolution 1.60Å" /> | ||
'''INHIBITION OF HIV-1 INFECTIVITY BY THE GP41 CORE: ROLE OF A CONSERVED HYDROPHOBIC CAVITY IN MEMBRANE FUSION'''<br /> | '''INHIBITION OF HIV-1 INFECTIVITY BY THE GP41 CORE: ROLE OF A CONSERVED HYDROPHOBIC CAVITY IN MEMBRANE FUSION'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1QR9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1]. Full crystallographic information is available from [http:// | + | 1QR9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1QR9 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: membrane fusion]] | [[Category: membrane fusion]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:45:54 2008'' |
Revision as of 14:45, 15 February 2008
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INHIBITION OF HIV-1 INFECTIVITY BY THE GP41 CORE: ROLE OF A CONSERVED HYDROPHOBIC CAVITY IN MEMBRANE FUSION
Overview
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.
About this Structure
1QR9 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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