2r5d: Difference between revisions

Revision as of 03:16, 28 July 2008

This article has been automatically seeded. Changes to this page should pertain to the PDB entry only and not to the protein or biomolecule in general.

File:2r5d.png

Template:STRUCTURE 2r5d

Structure of the gp41 N-trimer in complex with the HIV entry inhibitor PIE7Structure of the gp41 N-trimer in complex with the HIV entry inhibitor PIE7

Template:ABSTRACT PUBMED 17942675

About this StructureAbout this Structure

2R5D is a Protein complex structure. Full crystallographic information is available from OCA.

ReferenceReference

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

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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

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-'''Structure of the gp41 N-trimer in complex with the HIV entry inhibitor PIE7'''
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-==Overview==
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-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.
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 [[Category: Viral entry]]
 [[Category: Viral protein]]
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