2r3c

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[[Image:2r3c.gif|left|200px]]
[[Image:2r3c.gif|left|200px]]
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{{Structure
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|PDB= 2r3c |SIZE=350|CAPTION= <scene name='initialview01'>2r3c</scene>, resolution 1.730&Aring;
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The line below this paragraph, containing "STRUCTURE_2r3c", creates the "Structure Box" on the page.
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|SITE=
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|LIGAND= <scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=DAL:D-ALANINE'>DAL</scene>, <scene name='pdbligand=DCY:D-CYSTEINE'>DCY</scene>, <scene name='pdbligand=DGL:D-GLUTAMIC+ACID'>DGL</scene>, <scene name='pdbligand=DGN:D-GLUTAMINE'>DGN</scene>, <scene name='pdbligand=DLE:D-LEUCINE'>DLE</scene>, <scene name='pdbligand=DLY:D-LYSINE'>DLY</scene>, <scene name='pdbligand=DPR:D-PROLINE'>DPR</scene>, <scene name='pdbligand=DSN:D-SERINE'>DSN</scene>, <scene name='pdbligand=DTR:D-TRYPTOPHAN'>DTR</scene>, <scene name='pdbligand=NH2:AMINO+GROUP'>NH2</scene>, <scene name='pdbligand=YT3:YTTRIUM+(III)+ION'>YT3</scene>
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{{STRUCTURE_2r3c| PDB=2r3c | SCENE= }}
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|RELATEDENTRY=[[2r5b|2R5B]], [[2r5d|2R5D]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2r3c FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2r3c OCA], [http://www.ebi.ac.uk/pdbsum/2r3c PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2r3c RCSB]</span>
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'''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'''
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==About this Structure==
==About this Structure==
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2R3C is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/ ]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2R3C OCA].
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2R3C is a [[Protein complex]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2R3C OCA].
==Reference==
==Reference==
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[[Category: VanDemark, A P.]]
[[Category: VanDemark, A P.]]
[[Category: Welch, B.]]
[[Category: Welch, B.]]
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[[Category: hiv]]
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[[Category: Hiv]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: peptide]]
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[[Category: Peptide]]
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[[Category: pie]]
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[[Category: Pie]]
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[[Category: viral entry]]
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[[Category: Viral entry]]
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[[Category: viral protein]]
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[[Category: Viral protein]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 16:09:52 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:56:07 2008''
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Revision as of 13:09, 4 May 2008

Image:2r3c.gif

Template:STRUCTURE 2r3c

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. 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 16:09:52 2008

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