2r5b

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{{STRUCTURE_2r5b| PDB=2r5b | SCENE= }}
{{STRUCTURE_2r5b| PDB=2r5b | SCENE= }}
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'''Structure of the gp41 N-trimer in complex with the HIV entry inhibitor PIE7'''
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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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(as it appears on PubMed at http://www.pubmed.gov), where 17942675 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17942675}}
==About this Structure==
==About this Structure==
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[[Category: Viral entry]]
[[Category: Viral entry]]
[[Category: Viral protein]]
[[Category: Viral protein]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 16:16:40 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 09:46:50 2008''

Revision as of 06:46, 28 July 2008

Image:2r5b.png

Template:STRUCTURE 2r5b

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

Template:ABSTRACT PUBMED 17942675

About this Structure

2R5B 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

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