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2r3c

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(New page: 200px<br /><applet load="2r3c" size="350" color="white" frame="true" align="right" spinBox="true" caption="2r3c, resolution 1.730&Aring;" /> '''Structure of the gp...)
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Revision as of 10:20, 23 January 2008

Image:2r3c.gif

2r3c, resolution 1.730Å

Drag the structure with the mouse to rotate

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

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

2R3C is a Protein complex structure of sequences from [1] with , , and as ligands. 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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