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In vitro selection and molecular characterization of human immunodeficiency virus-1 resistant to non-nucleoside inhibitors of reverse transcriptase

MELLORS, J. W ; DUTSCHMAN, G. E ; GUANG-JIN IM ; TRAMONTANO, E ; WINKLER, S. R ; YUNG-CHI CHENG

Molecular pharmacology, 1992-03, Vol.41 (3), p.446-451 [Periódico revisado por pares]

Bethesda, MD: American Society for Pharmacology and Experimental Therapeutics

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Título:
In vitro selection and molecular characterization of human immunodeficiency virus-1 resistant to non-nucleoside inhibitors of reverse transcriptase
Autor: MELLORS, J. W ; DUTSCHMAN, G. E ; GUANG-JIN IM ; TRAMONTANO, E ; WINKLER, S. R ; YUNG-CHI CHENG
Assuntos: Action of physical and chemical agents ; AIDS/HIV ; Antiviral Agents - pharmacology ; Base Sequence ; Benzodiazepines - pharmacology ; Biological and medical sciences ; CD4-Positive T-Lymphocytes - drug effects ; CD4-Positive T-Lymphocytes - microbiology ; Cloning, Molecular ; Drug Resistance, Microbial ; Foscarnet ; Fundamental and applied biological sciences. Psychology ; Gene Expression ; HeLa Cells ; HIV-1 - drug effects ; HIV-1 - enzymology ; HIV-1 - isolation & purification ; Humans ; Imidazoles - pharmacology ; Microbiology ; Molecular Sequence Data ; Nevirapine ; Phosphonoacetic Acid - analogs & derivatives ; Phosphonoacetic Acid - pharmacology ; Polymerase Chain Reaction ; Pyridines - pharmacology ; Recombinant Proteins - antagonists & inhibitors ; Recombinant Proteins - genetics ; Reverse Transcriptase Inhibitors ; RNA-Directed DNA Polymerase - genetics ; Virology ; Zidovudine - analogs & derivatives ; Zidovudine - pharmacology
É parte de: Molecular pharmacology, 1992-03, Vol.41 (3), p.446-451
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SourceType-Scholarly Journals-1
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Descrição: Several newly discovered potent and selective non-nucleoside inhibitors of human immunodeficiency virus-1 reverse transcriptase (RT) are undergoing evaluation in clinical trials. We studied the potential for development of viral resistance to one of the prototype compounds, BI-RG-587, a dipyridodiazepinone derivative. Human immunodeficiency virus-1 resistant to BI-RG-587 emerged after only one cycle of in vitro infection in the presence of the drug. Resistant virus was cross-resistant to the non-nucleoside tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-thione derivative R82150 but remained susceptible to 2',3'-dideoxynucleosides and phosphonoformate. Both native (virion-associated) and recombinant RT derived from resistant virus were insensitive to BI-RG-587 and R82150. Nucleotide sequence analysis of multiple drug-resistant and -sensitive recombinant RT clones identified a single predicted amino acid change common to all resistant clones (tyrosine-181---cysteine). These studies suggest that the viral resistance to non-nucleoside RT inhibitors may develop in vivo. This possibility should be carefully monitored in clinical trials of these compounds.
Editor: Bethesda, MD: American Society for Pharmacology and Experimental Therapeutics
Idioma: Inglês

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In vitro selection and molecular characterization of human immunodeficiency virus-1 resistant to non-nucleoside inhibitors of reverse transcriptase

MELLORS, J. W ; DUTSCHMAN, G. E ; GUANG-JIN IM ; TRAMONTANO, E ; WINKLER, S. R ; YUNG-CHI CHENG

Bethesda, MD: American Society for Pharmacology and Experimental Therapeutics

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