2r3c: Difference between revisions

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[[Image:2r3c.gif|left|200px]]
{{Seed}}
[[Image:2r3c.png|left|200px]]


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{{STRUCTURE_2r3c|  PDB=2r3c  |  SCENE=  }}  
{{STRUCTURE_2r3c|  PDB=2r3c  |  SCENE=  }}  


'''Structure of the gp41 N-peptide in complex with the HIV entry inhibitor PIE1'''
===Structure of the gp41 N-peptide in complex with the HIV entry inhibitor PIE1===




==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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{{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]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 16:09:52 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 02:12:58 2008''

Revision as of 23:13, 28 July 2008

File:2r3c.png

Template:STRUCTURE 2r3c

Structure of the gp41 N-peptide in complex with the HIV entry inhibitor PIE1

Template:ABSTRACT PUBMED 17942675

About this Structure

2R3C 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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