1rtj
From Proteopedia
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| - | [[Image:1rtj.jpg|left|200px]] | + | [[Image:1rtj.jpg|left|200px]] |
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| - | '''MECHANISM OF INHIBITION OF HIV-1 REVERSE TRANSCRIPTASE BY NON-NUCLEOSIDE INHIBITORS''' | + | {{Structure |
| + | |PDB= 1rtj |SIZE=350|CAPTION= <scene name='initialview01'>1rtj</scene>, resolution 2.35Å | ||
| + | |SITE= | ||
| + | |LIGAND= <scene name='pdbligand=CYA:TWO OXYGEN ATOMS BOUND TO SG OF CYS'>CYA</scene> | ||
| + | |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] | ||
| + | |GENE= HIV-1 POL ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=11676 Human immunodeficiency virus 1]) | ||
| + | }} | ||
| + | |||
| + | '''MECHANISM OF INHIBITION OF HIV-1 REVERSE TRANSCRIPTASE BY NON-NUCLEOSIDE INHIBITORS''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1RTJ is a [ | + | 1RTJ 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=1RTJ OCA]. |
==Reference== | ==Reference== | ||
| - | Mechanism of inhibition of HIV-1 reverse transcriptase by non-nucleoside inhibitors., Esnouf R, Ren J, Ross C, Jones Y, Stammers D, Stuart D, Nat Struct Biol. 1995 Apr;2(4):303-8. PMID:[http:// | + | Mechanism of inhibition of HIV-1 reverse transcriptase by non-nucleoside inhibitors., Esnouf R, Ren J, Ross C, Jones Y, Stammers D, Stuart D, Nat Struct Biol. 1995 Apr;2(4):303-8. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/7540935 7540935] |
[[Category: Human immunodeficiency virus 1]] | [[Category: Human immunodeficiency virus 1]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
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[[Category: hiv-1 reverse transcriptase]] | [[Category: hiv-1 reverse transcriptase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 13:56:00 2008'' |
Revision as of 11:56, 20 March 2008
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| , resolution 2.35Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | HIV-1 POL (Human immunodeficiency virus 1) | ||||||
| Activity: | RNA-directed DNA polymerase, with EC number 2.7.7.49 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
MECHANISM OF INHIBITION OF HIV-1 REVERSE TRANSCRIPTASE BY NON-NUCLEOSIDE INHIBITORS
Overview
The structure of unliganded HIV-1 reverse transcriptase has been determined at 2.35 A resolution and refined to an R-factor of 0.219 (for all data) with good stereochemistry. The unliganded structure was produced by soaking out a weak binding non-nucleoside inhibitor, HEPT, from pregrown crystals. Comparison with the structures of four different RT and non-nucleoside inhibitor complexes reveals that only minor domain rearrangements occur, but there is a significant repositioning of a three-stranded beta-sheet in the p66 subunit (containing the catalytic aspartic acid residues 110, 185 and 186) with respect to the rest of the polymerase site. This suggests that NNIs inhibit RT by locking the polymerase active site in an inactive conformation, reminiscent of the conformation observed in the inactive p51 subunit.
About this Structure
1RTJ is a Protein complex structure of sequences from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.
Reference
Mechanism of inhibition of HIV-1 reverse transcriptase by non-nucleoside inhibitors., Esnouf R, Ren J, Ross C, Jones Y, Stammers D, Stuart D, Nat Struct Biol. 1995 Apr;2(4):303-8. PMID:7540935
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