1rtj
From Proteopedia
(New page: 200px<br /> <applet load="1rtj" size="450" color="white" frame="true" align="right" spinBox="true" caption="1rtj, resolution 2.35Å" /> '''MECHANISM OF INHIBI...) |
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caption="1rtj, resolution 2.35Å" /> | caption="1rtj, resolution 2.35Å" /> | ||
'''MECHANISM OF INHIBITION OF HIV-1 REVERSE TRANSCRIPTASE BY NON-NUCLEOSIDE INHIBITORS'''<br /> | '''MECHANISM OF INHIBITION OF HIV-1 REVERSE TRANSCRIPTASE BY NON-NUCLEOSIDE INHIBITORS'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1RTJ 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 CYA as [http://en.wikipedia.org/wiki/ligand ligand]. 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:// | + | 1RTJ 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=CYA:'>CYA</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. 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=1RTJ OCA]. |
==Reference== | ==Reference== | ||
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[[Category: hiv-1 reverse transcriptase]] | [[Category: hiv-1 reverse transcriptase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:50:03 2008'' |
Revision as of 14:50, 15 February 2008
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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 with as ligand. Active as RNA-directed DNA polymerase, with EC number 2.7.7.49 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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