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77953871966
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note
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Atomic coordinates for the structures of Etravirine and 5h bound to HIV/RT have been deposited with the RCSB Protein Data Bank (PDB) under the access codes 3M8P, and 3M8Q, respectively.
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13
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77953869982
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note
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50 values were obtained from a SPA heteropolymeric assay. RNA-dependent DNA polymerase activity was measured using a biotinylated primer oligonucleotide and tritiated dNTP substrate. Newly synthesized DNA was quantified by capturing the biotinylated primer molecules on streptavidin coated Scintillation Proximity Assay (SPA) beads (Amersham).
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14
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77953870422
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For a detailed description of the syntheses of aminopyrimidine inhibitors see: Kertesz, D. J.; Brotherton-Pleiss, C.; Yang, M. US 2008/0146595.
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For a detailed description of the syntheses of aminopyrimidine inhibitors see: Kertesz, D. J.; Brotherton-Pleiss, C.; Yang, M. US 2008/0146595.
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15
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0023277417
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50 values were obtained following incubation of compound with infected MT4 cells in the presence of 10% fetal bovine serum (FBS). The assay assesses the reduction in the cytopathic effect of HIV-1 on MT4 cells in the presence of HIV-RT inhibitors. Each value represents the average of at least two independent assays. For a detailed description of the anitiviral assay see:
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50 values were obtained following incubation of compound with infected MT4 cells in the presence of 10% fetal bovine serum (FBS). The assay assesses the reduction in the cytopathic effect of HIV-1 on MT4 cells in the presence of HIV-RT inhibitors. Each value represents the average of at least two independent assays. For a detailed description of the anitiviral assay see:. Pauwels R., De C.E., Desmyter J., Balzarini J., Goubau P., Herdewijn P., Vanderhaeghe H., and Vandeputte M. J. Virol. Methods 16 (1987) 171
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16
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0027466031
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Carroll S.S., Olsen D.B., Bennett C.D., Gotlib L., Graham D.J., Condra J.H., Stern A.M., Shafer J.A., and Kuo L.C. J. Biol. Chem. 268 (1993) 276
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17
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77953871573
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note
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Determination of potency versus wild type virus was repeated in the presence of 40% human serum (HS) for these compounds. The resulting 'protein shifted potency' as compared to the result with 10% FBS (see Ref. 15) is considered an indicator of potential for in vivo activity.
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