1uts: Difference between revisions

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[[Image:1uts.gif|left|200px]]
{{Seed}}
[[Image:1uts.png|left|200px]]


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{{STRUCTURE_1uts|  PDB=1uts  |  SCENE=  }}  
{{STRUCTURE_1uts|  PDB=1uts  |  SCENE=  }}  


'''DESIGNED HIV-1 TAR BINDING LIGAND'''
===DESIGNED HIV-1 TAR BINDING LIGAND===




==Overview==
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The targeting of RNA for the design of novel anti-viral compounds represents an area of vast potential. We have used NMR and computational methods to model the interaction of a series of synthetic inhibitors of the in vitro RNA binding activities of a peptide derived from the transcriptional activator protein, Tat, from human immunodeficiency virus type 1. Inhibition has been measured through the monitering of fluorescence resonance energy transfer between fluorescently labeled peptide and RNA components. A series of compounds containing a bi-aryl heterocycle as one of the three substituents on a benzylic scaffold, induce a novel, inactive TAR conformation by stacking between base-pairs at the site of a three-base bulge within TAR. The development of this series resulted in an enhancement in potency (with Ki &lt; 100 nM in an in vitro assay) and the removal of problematic guanidinium moieties. Ligands from this series can act as inhibitors of Tat-induced transcription in a cell-free system. This study validates the drug design strategy of using a ligand to target the RNA receptor in a non-functional conformation.
The line below this paragraph, {{ABSTRACT_PUBMED_15095977}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 15095977 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15095977}}


==About this Structure==
==About this Structure==
1UTS is a [[Single protein]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1UTS OCA].  
1UTS is a [[Single protein]] structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1UTS OCA].  


==Reference==
==Reference==
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[[Category: Ligand binding]]
[[Category: Ligand binding]]
[[Category: Tar rna]]
[[Category: Tar rna]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 11:40:48 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 23:13:29 2008''

Revision as of 20:13, 27 July 2008

File:1uts.png

Template:STRUCTURE 1uts

DESIGNED HIV-1 TAR BINDING LIGAND

Template:ABSTRACT PUBMED 15095977

About this Structure

1UTS is a Single protein structure. Full experimental information is available from OCA.

Reference

Structure-based drug design targeting an inactive RNA conformation: exploiting the flexibility of HIV-1 TAR RNA., Murchie AI, Davis B, Isel C, Afshar M, Drysdale MJ, Bower J, Potter AJ, Starkey ID, Swarbrick TM, Mirza S, Prescott CD, Vaglio P, Aboul-ela F, Karn J, J Mol Biol. 2004 Feb 20;336(3):625-38. PMID:15095977

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