1ep4
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(New page: 200px<br /> <applet load="1ep4" size="450" color="white" frame="true" align="right" spinBox="true" caption="1ep4, resolution 2.5Å" /> '''CRYSTAL STRUCTURE OF...)
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Revision as of 11:55, 8 November 2007
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CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH S-1153
Overview
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
1EP4 is a Protein complex structure of sequences from Human immunodeficiency virus 1 with S11 as ligand. Active as RNA-directed DNA polymerase, with EC number 2.7.7.49 Full crystallographic information is available from OCA.
Reference
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
Page seeded by OCA on Thu Nov 8 14:01:14 2007
