1t05

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[[Image:1t05.gif|left|200px]]<br /><applet load="1t05" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1t05.gif|left|200px]]
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caption="1t05, resolution 3.0&Aring;" />
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'''HIV-1 reverse transcriptase crosslinked to template-primer with tenofovir-diphosphate bound as the incoming nucleotide substrate'''<br />
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{{Structure
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|PDB= 1t05 |SIZE=350|CAPTION= <scene name='initialview01'>1t05</scene>, resolution 3.0&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=TNV:[2-(6-AMINO-9H-PURIN-9-YL)-1-METHYLETHOXY]METHYL-TRIPHOSPHATE'>TNV</scene> and <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/RNA-directed_DNA_polymerase RNA-directed DNA polymerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.7.49 2.7.7.49]
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|GENE= POL ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=11676 Human immunodeficiency virus 1])
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}}
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'''HIV-1 reverse transcriptase crosslinked to template-primer with tenofovir-diphosphate bound as the incoming nucleotide substrate'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1T05 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1] with <scene name='pdbligand=MG:'>MG</scene>, <scene name='pdbligand=TNV:'>TNV</scene> and <scene name='pdbligand=GOL:'>GOL</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/RNA-directed_DNA_polymerase RNA-directed DNA polymerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.7.49 2.7.7.49] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1T05 OCA].
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1T05 is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1T05 OCA].
==Reference==
==Reference==
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Structures of HIV-1 RT-DNA complexes before and after incorporation of the anti-AIDS drug tenofovir., Tuske S, Sarafianos SG, Clark AD Jr, Ding J, Naeger LK, White KL, Miller MD, Gibbs CS, Boyer PL, Clark P, Wang G, Gaffney BL, Jones RA, Jerina DM, Hughes SH, Arnold E, Nat Struct Mol Biol. 2004 May;11(5):469-74. Epub 2004 Apr 25. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15107837 15107837]
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Structures of HIV-1 RT-DNA complexes before and after incorporation of the anti-AIDS drug tenofovir., Tuske S, Sarafianos SG, Clark AD Jr, Ding J, Naeger LK, White KL, Miller MD, Gibbs CS, Boyer PL, Clark P, Wang G, Gaffney BL, Jones RA, Jerina DM, Hughes SH, Arnold E, Nat Struct Mol Biol. 2004 May;11(5):469-74. Epub 2004 Apr 25. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15107837 15107837]
[[Category: Human immunodeficiency virus 1]]
[[Category: Human immunodeficiency virus 1]]
[[Category: Protein complex]]
[[Category: Protein complex]]
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[[Category: tenofovir]]
[[Category: tenofovir]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:08:16 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 14:11:52 2008''

Revision as of 12:11, 20 March 2008

Image:1t05.gif


PDB ID 1t05

Drag the structure with the mouse to rotate
, resolution 3.0Å
Ligands: , and
Gene: POL (Human immunodeficiency virus 1)
Activity: RNA-directed DNA polymerase, with EC number 2.7.7.49
Coordinates: save as pdb, mmCIF, xml



HIV-1 reverse transcriptase crosslinked to template-primer with tenofovir-diphosphate bound as the incoming nucleotide substrate


Overview

Tenofovir, also known as PMPA, R-9-(2-(phosphonomethoxypropyl)adenine, is a nucleotide reverse transcriptase (RT) inhibitor. We have determined the crystal structures of two related complexes of HIV-1 RT with template primer and tenofovir: (i) a ternary complex at a resolution of 3.0 A of RT crosslinked to a dideoxy-terminated DNA with tenofovir-diphosphate bound as the incoming substrate; and (ii) a RT-DNA complex at a resolution of 3.1 A with tenofovir at the 3' primer terminus. The tenofovir nucleotide in the tenofovir-terminated structure seems to adopt multiple conformations. Some nucleoside reverse transcriptase inhibitors, including 3TC and AZT, have elements ('handles') that project beyond the corresponding elements on normal dNTPs (the 'substrate envelope'). HIV-1 RT resistance mechanisms to AZT and 3TC take advantage of these handles; tenofovir's structure lacks handles that could protrude through the substrate envelope to cause resistance.

About this Structure

1T05 is a Protein complex structure of sequences from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.

Reference

Structures of HIV-1 RT-DNA complexes before and after incorporation of the anti-AIDS drug tenofovir., Tuske S, Sarafianos SG, Clark AD Jr, Ding J, Naeger LK, White KL, Miller MD, Gibbs CS, Boyer PL, Clark P, Wang G, Gaffney BL, Jones RA, Jerina DM, Hughes SH, Arnold E, Nat Struct Mol Biol. 2004 May;11(5):469-74. Epub 2004 Apr 25. PMID:15107837

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