1ep4: Difference between revisions
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==Overview== | ==Overview== | ||
S-1153 (AG1549) is perhaps the most promising non-nucleoside inhibitor of | S-1153 (AG1549) is perhaps the most promising non-nucleoside inhibitor of HIV-1 reverse transcriptase currently under development as a potential anti-AIDS drug, because it has a favorable profile of resilience to many drug resistance mutations. We have determined the crystal structure of S-1153 in a complex with HIV-1 reverse transcriptase. The complex possesses some novel features, including an extensive network of hydrogen bonds involving the main chain of residues 101, 103, and 236 of the p66 reverse transcriptase subunit. Such interactions are unlikely to be disrupted by side chain mutations. The reverse transcriptase/S-1153 complex suggests different ways in which resilience to mutations in the non-nucleoside inhibitors of reverse transcriptase binding site can be achieved. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: RNA-directed DNA polymerase]] | [[Category: RNA-directed DNA polymerase]] | ||
[[Category: Bird, L | [[Category: Bird, L E.]] | ||
[[Category: Fujiwara, T.]] | [[Category: Fujiwara, T.]] | ||
[[Category: Nichols, C.]] | [[Category: Nichols, C.]] | ||
[[Category: Ren, J.]] | [[Category: Ren, J.]] | ||
[[Category: Stammers, D | [[Category: Stammers, D K.]] | ||
[[Category: Stuart, D | [[Category: Stuart, D I.]] | ||
[[Category: Suginoto, H.]] | [[Category: Suginoto, H.]] | ||
[[Category: S11]] | [[Category: S11]] | ||
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[[Category: s-1153]] | [[Category: s-1153]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:30:05 2008'' | ||
Revision as of 13:30, 21 February 2008
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CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH S-1153
OverviewOverview
S-1153 (AG1549) is perhaps the most promising non-nucleoside inhibitor of HIV-1 reverse transcriptase currently under development as a potential anti-AIDS drug, because it has a favorable profile of resilience to many drug resistance mutations. We have determined the crystal structure of S-1153 in a complex with HIV-1 reverse transcriptase. The complex possesses some novel features, including an extensive network of hydrogen bonds involving the main chain of residues 101, 103, and 236 of the p66 reverse transcriptase subunit. Such interactions are unlikely to be disrupted by side chain mutations. The reverse transcriptase/S-1153 complex suggests different ways in which resilience to mutations in the non-nucleoside inhibitors of reverse transcriptase binding site can be achieved.
About this StructureAbout this Structure
1EP4 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.
ReferenceReference
Binding of the second generation non-nucleoside inhibitor S-1153 to HIV-1 reverse transcriptase involves extensive main chain hydrogen bonding., Ren J, Nichols C, Bird LE, Fujiwara T, Sugimoto H, Stuart DI, Stammers DK, J Biol Chem. 2000 May 12;275(19):14316-20. PMID:10799511
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