Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells

Science

Volumn 287, Issue 5453, 2000, Pages 646-650

  Hazuda, Daria J ^a   Felock, Peter ^a   Witmer, Marc ^a   Wolfe, Abigail ^a   Stillmock, Kara ^a   Grobler, Jay A ^a   Espeseth, Amy ^a   Gabryelski, Lori ^a   Schleif, William ^a   Blau, Carol ^a   Miller, Michael D ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIRETROVIRUS AGENT; INTEGRASE; L 708 906; L 731 988; UNCLASSIFIED DRUG; VIRUS DNA;

ANTIVIRAL ACTIVITY; ARTICLE; DNA TRANSFER; DRUG EFFECT; ENZYME INHIBITION; GENE MUTATION; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; IC 50; NONHUMAN; PRIORITY JOURNAL; VIRUS DNA CELL DNA INTERACTION; VIRUS REPLICATION;

ACETOACETATES; ANTI-HIV AGENTS; CATALYSIS; COCULTURE TECHNIQUES; DNA, CIRCULAR; DNA, VIRAL; DRUG RESISTANCE, MICROBIAL; HIV INTEGRASE; HIV INTEGRASE INHIBITORS; HIV LONG TERMINAL REPEAT; HIV-1; HUMANS; MUTATION; PYRROLES; RECOMBINANT PROTEINS; T-LYMPHOCYTES; TRANSCRIPTION, GENETIC; TUMOR CELLS, CULTURED; VIRUS INTEGRATION; VIRUS REPLICATION;

DNA VIRUSES; HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 0034723439     PISSN: 00368075     EISSN: None     Source Type: Journal    
DOI: 10.1126/science.287.5453.646     Document Type: Article

References (30)

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21. M. Witmer, W. Schleif, P. Felock, A. Wolfe, D. J. Hazuda, unpublished observations.
22. The disintegration reaction is a catalytic activity that represents the reverse of strand transfer [S. A. Chow, K. A. Vincent, V. Ellison, P. O. Brown, Science 255, 723 (1992)].
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27. The L-708,906-resistant population (L-708,906R) was derived from HIV-1 IIIB in H9 cells after eight passages: two passages at 3 μM L-708,906, one passage at 5 μM, three passages at 10 μM, and one passage at 20 μM. The L-731,988-resistant population (L-731,988R) was similarly derived after 10 passages: 2 passages at 3 μM, 5 passages at 6 μM, 2 passages at 12 μM, and 1 passage at 25 μM, RNA derived from these variants and the wild-type IIIB was used to make cDNA for sequence analysis (Table 1).
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30. We thank E. Emini, J. Condra, and M. Shivaprakash for their advice and assistance.