1t05

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[[Image:1t05.gif|left|200px]]
[[Image:1t05.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1t05 |SIZE=350|CAPTION= <scene name='initialview01'>1t05</scene>, resolution 3.0&Aring;
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The line below this paragraph, containing "STRUCTURE_1t05", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=DA:2&#39;-DEOXYADENOSINE-5&#39;-MONOPHOSPHATE'>DA</scene>, <scene name='pdbligand=DC:2&#39;-DEOXYCYTIDINE-5&#39;-MONOPHOSPHATE'>DC</scene>, <scene name='pdbligand=DDG:2&#39;,3&#39;-DIDEOXY-GUANOSINE-5&#39;-MONOPHOSPHATE'>DDG</scene>, <scene name='pdbligand=DG:2&#39;-DEOXYGUANOSINE-5&#39;-MONOPHOSPHATE'>DG</scene>, <scene name='pdbligand=DT:THYMIDINE-5&#39;-MONOPHOSPHATE'>DT</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=MRG:N2-(3-MERCAPTOPROPYL)-2&#39;-DEOXYGUANOSINE-5&#39;-MONOPHOSPHATE'>MRG</scene>, <scene name='pdbligand=TNV:[2-(6-AMINO-9H-PURIN-9-YL)-1-METHYLETHOXY]METHYL-TRIPHOSPHATE'>TNV</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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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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|DOMAIN=
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{{STRUCTURE_1t05| PDB=1t05 | SCENE= }}
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|RELATEDENTRY=[[1rtd|1RTD]], [[1t03|1T03]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1t05 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1t05 OCA], [http://www.ebi.ac.uk/pdbsum/1t05 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1t05 RCSB]</span>
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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'''
'''HIV-1 reverse transcriptase crosslinked to template-primer with tenofovir-diphosphate bound as the incoming nucleotide substrate'''
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[[Category: Sarafianos, S G.]]
[[Category: Sarafianos, S G.]]
[[Category: Tuske, S.]]
[[Category: Tuske, S.]]
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[[Category: hiv-1 reverse transcriptase]]
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[[Category: Hiv-1 reverse transcriptase]]
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[[Category: rt-dna complex]]
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[[Category: Rt-dna complex]]
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[[Category: tenofovir]]
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[[Category: Tenofovir]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 09:20:17 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:49:17 2008''
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Revision as of 06:20, 3 May 2008

Image:1t05.gif

Template:STRUCTURE 1t05

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 Page seeded by OCA on Sat May 3 09:20:17 2008

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