1rev

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{{STRUCTURE_1rev| PDB=1rev | SCENE= }}
{{STRUCTURE_1rev| PDB=1rev | SCENE= }}
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'''HIV-1 REVERSE TRANSCRIPTASE'''
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===HIV-1 REVERSE TRANSCRIPTASE===
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==Overview==
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BACKGROUND: HIV reverse transcriptase (RT) is a key target of anti-AIDS therapies. Structural studies of HIV-1 RT, unliganded and complexed with different non-nucleoside inhibitors (NNIs), have pointed to a common mode of binding and inactivation through distortion of the polymerase catalytic site by NNIs containing two hinged rings. The mode of binding of the TIBO family of inhibitors is of interest because these compounds do not fit the two-hinged-ring model. RESULTS: The structure of HIV-1 RT complexed with 9-chloro-TIBO (R82913) has been determined at 2.6 A resolution. As reported for the lower resolution analysis of another TIBO compound, this inhibitor binds at the same site as other NNIs, but our higher resolution study reveals the Cl-TIBO is distorted from the conformation seen in crystals of the inhibitor alone. This allows Cl-TIBO to mimic the binding of NNIs containing two hinged rings. Inhibitor-protein interactions are again predominantly hydrophobic and the protein conformation corresponds to that seen in complexes with other tight-binding NNIs. CONCLUSIONS: Although Cl-TIBO is chemically very different from other NNIs, it achieves remarkable spatial equivalence and shape complementarity with other NNIs on binding to RT. Comparison of the different RT-NNI complexes suggests modifications to the TIBO group of inhibitors which might enhance their binding and hence, potentially, their therapeutic efficacy.
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(as it appears on PubMed at http://www.pubmed.gov), where 8535785 is the PubMed ID number.
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{{ABSTRACT_PUBMED_8535785}}
==About this Structure==
==About this Structure==
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[[Category: Nucleotidyltransferase]]
[[Category: Nucleotidyltransferase]]
[[Category: Polyprotein]]
[[Category: Polyprotein]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 07:24:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 09:14:53 2008''

Revision as of 06:14, 28 July 2008

Image:1rev.png

Template:STRUCTURE 1rev

HIV-1 REVERSE TRANSCRIPTASE

Template:ABSTRACT PUBMED 8535785

About this Structure

1REV is a Protein complex structure of sequences from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.

Reference

The structure of HIV-1 reverse transcriptase complexed with 9-chloro-TIBO: lessons for inhibitor design., Ren J, Esnouf R, Hopkins A, Ross C, Jones Y, Stammers D, Stuart D, Structure. 1995 Sep 15;3(9):915-26. PMID:8535785

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