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2r5d
From Proteopedia
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[[Image:2r5d.jpg|left|200px]] | [[Image:2r5d.jpg|left|200px]] | ||
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'''Structure of the gp41 N-trimer in complex with the HIV entry inhibitor PIE7''' | '''Structure of the gp41 N-trimer in complex with the HIV entry inhibitor PIE7''' | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2R5D is a [[Protein complex]] structure | + | 2R5D is a [[Protein complex]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2R5D OCA]. |
==Reference== | ==Reference== | ||
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[[Category: VanDemark, A P.]] | [[Category: VanDemark, A P.]] | ||
[[Category: Welch, B.]] | [[Category: Welch, B.]] | ||
| - | [[Category: | + | [[Category: Hiv]] |
| - | [[Category: | + | [[Category: Inhibitor]] |
| - | [[Category: | + | [[Category: Peptide]] |
| - | [[Category: | + | [[Category: Pie]] |
| - | [[Category: | + | [[Category: Viral entry]] |
| - | [[Category: | + | [[Category: Viral protein]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 16:16:43 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 13:16, 4 May 2008
Structure of the gp41 N-trimer in complex with the HIV entry inhibitor PIE7
Overview
During HIV-1 entry, the highly conserved gp41 N-trimer pocket region becomes transiently exposed and vulnerable to inhibition. Using mirror-image phage display and structure-assisted design, we have discovered protease-resistant D-amino acid peptides (D-peptides) that bind the N-trimer pocket with high affinity and potently inhibit viral entry. We also report high-resolution crystal structures of two of these D-peptides in complex with a pocket mimic that suggest sources of their high potency. A trimeric version of one of these peptides is the most potent pocket-specific entry inhibitor yet reported by three orders of magnitude (IC(50) = 250 pM). These results are the first demonstration that D-peptides can form specific and high-affinity interactions with natural protein targets and strengthen their promise as therapeutic agents. The D-peptides described here address limitations associated with current L-peptide entry inhibitors and are promising leads for the prevention and treatment of HIV/AIDS.
About this Structure
2R5D is a Protein complex structure. Full crystallographic information is available from OCA.
Reference
Potent D-peptide inhibitors of HIV-1 entry., Welch BD, VanDemark AP, Heroux A, Hill CP, Kay MS, Proc Natl Acad Sci U S A. 2007 Oct 23;104(43):16828-33. Epub 2007 Oct 17. PMID:17942675 Page seeded by OCA on Sun May 4 16:16:43 2008
Categories: Protein complex | Heroux, A. | Hill, C P. | Kay, M S. | VanDemark, A P. | Welch, B. | Hiv | Inhibitor | Peptide | Pie | Viral entry | Viral protein
