منابع مشابه
HIV Nucleoside Reverse Transcriptase Inhibitors
Currently, 16 antiretroviral drugs are approved for treatment of HIV infection. However, even the best currently available regimens pose challenges with regard to adherence, toxicity, antiviral activity, and resistance. New drug development thus confronts the need for improved convenience and tolerability, reduced toxicity, and improved activity against both wild-type and drug-resistant viruses...
متن کاملNonnucleoside reverse transcriptase inhibitors are chemical enhancers of dimerization of the HIV type 1 reverse transcriptase.
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are allosteric inhibitors of the HIV type 1 (HIV-1) reverse transcriptase (RT). Yeast grown in the presence of many of these drugs exhibited dramatically increased association of the p66 and p51 subunits of the HIV-1 RT as reported by a yeast two-hybrid assay. The enhancement required drug binding by RT; introduction of a drug-resistance m...
متن کاملNucleoside reverse transcriptase inhibitors and HIV mutagenesis.
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متن کاملConformational changes in HIV-1 reverse transcriptase induced by nonnucleoside reverse transcriptase inhibitor binding.
Nonnucleoside reverse transcriptase inhibitors (NNRTI) are a group of small hydrophobic compounds with diverse structures that specifically inhibit HIV-1 reverse transcriptase (RT). NNRTIs interact with HIV-1 RT by binding to a single site on the p66 subunit of the p66/p51 heterodimeric enzyme, termed the NNRTI-binding pocket (NNRTI-BP). This binding interaction results in both short-range and ...
متن کاملStructure of a covalently trapped catalytic complex of HIV-1 reverse transcriptase: implications for drug resistance.
A combinatorial disulfide cross-linking strategy was used to prepare a stalled complex of human immunodeficiency virus-type 1 (HIV-1) reverse transcriptase with a DNA template:primer and a deoxynucleoside triphosphate (dNTP), and the crystal structure of the complex was determined at a resolution of 3.2 angstroms. The presence of a dideoxynucleotide at the 3'-primer terminus allows capture of a...
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ژورنال
عنوان ژورنال: Acta Crystallographica Section A Foundations of Crystallography
سال: 1993
ISSN: 0108-7673
DOI: 10.1107/s0108767378095598