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| | {{STRUCTURE_2a9x| PDB=2a9x | SCENE= }} | | {{STRUCTURE_2a9x| PDB=2a9x | SCENE= }} |
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| - | '''TAR RNA recognition by a cyclic peptidomimetic of Tat protein'''
| + | ===TAR RNA recognition by a cyclic peptidomimetic of Tat protein=== |
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| - | ==Overview==
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| - | The search for new antiviral drugs that repress HIV viral replication by blocking transactivation of viral RNA transcription has long been advocated as an approach to novel antiviral therapy. However, research in this area has so far failed to yield attractive lead compounds because of the insufficient development of RNA-based medicinal chemistry. One difficulty in efforts to inhibit protein-RNA interactions using small druglike molecules is the large surface areas typically found at these interfaces. To overcome this problem, we sought to identify constrained peptidomimetic inhibitors that would provide potential new drug leads. We previously reported the discovery of a cyclic peptide mimic of the RNA-binding domain of BIV Tat protein based on a designed beta-hairpin scaffold. We demonstrated that the cyclic peptide bound BIV TAR RNA with an affinity comparable to that of the RNA-binding domain of the Tat protein and inhibited protein binding to the RNA. In this study, we report the structure of the complex of the cyclic peptide bound to BIV TAR RNA determined using heteronuclear NMR methods. The structure reveals a beta-hairpin conformation in the bound peptide, which adopts an unexpected orientation in the major groove of the RNA opposite those observed for peptides derived from the Tat protein. This structure suggests many ways in which to optimize the compound and enhance its activity and pharmacological potential and represents a further step in the rational design of a new class of HIV-1 virus replication inhibitors based on peptidomimetic chemistry. | + | The line below this paragraph, {{ABSTRACT_PUBMED_16156649}}, adds the Publication Abstract to the page |
| | + | (as it appears on PubMed at http://www.pubmed.gov), where 16156649 is the PubMed ID number. |
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| | + | {{ABSTRACT_PUBMED_16156649}} |
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| | ==About this Structure== | | ==About this Structure== |
| - | Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2A9X OCA]. | + | Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2A9X OCA]. |
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| | ==Reference== | | ==Reference== |
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| | [[Category: Rna recognition]] | | [[Category: Rna recognition]] |
| | [[Category: Tar rna;]] | | [[Category: Tar rna;]] |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 18:47:34 2008'' | + | |
| | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 07:32:31 2008'' |
Revision as of 04:32, 29 July 2008
Template:STRUCTURE 2a9x
TAR RNA recognition by a cyclic peptidomimetic of Tat protein
Template:ABSTRACT PUBMED 16156649
About this Structure
Full experimental information is available from OCA.
Reference
TAR RNA recognition by a cyclic peptidomimetic of Tat protein., Leeper TC, Athanassiou Z, Dias RL, Robinson JA, Varani G, Biochemistry. 2005 Sep 20;44(37):12362-72. PMID:16156649
Page seeded by OCA on Tue Jul 29 07:32:31 2008
