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J Balzarini M J Pérez-Pérez A San-Félix M J Camarasa I C Bathurst P J Barr E De Clercq 《The Journal of biological chemistry》1992,267(17):11831-11838
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The phenylmethylthiazolylthiourea nonnucleoside reverse transcriptase (RT) inhibitor MSK-076 selects for a resistance mutation in the active site of human immunodeficiency virus type 2 RT
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Auwerx J Stevens M Van Rompay AR Bird LE Ren J De Clercq E Oberg B Stammers DK Karlsson A Balzarini J 《Journal of virology》2004,78(14):7427-7437
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A series of d4T di‐ or triphosphate derivatives have been synthesized and evaluated as effective substrates for HIV‐1 RT, and also tested for their in vitro anti‐HIV activity. The steady‐state kinetic study of compounds 1 – 4 in an enzymatic incorporation assay by HIV‐1 RT follows Michaelis? Menten profile. In addition, compounds 2 – 4 are able to inhibit HIV‐1 replication to the same extent as d4T and d4TMP in MT‐4 cells, as well as in CEM/0 cells and CEM/TK? cells. The data suggests that these d4T polyphosphate derivatives are hydrolyzed to d4T and rephosphorylated to d4TTP before exerting their antiviral activity. 相似文献
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Cases-González CE Franco S Martínez MA Menéndez-Arias L 《Journal of molecular biology》2007,365(2):298-309
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Hameau L Jeusset J Lafosse S Coulaud D Delain E Unge T Restle T Le Cam E Mirambeau G 《Journal of virology》2001,75(7):3301-3313
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