Steady-state kinetic studies with the polysulfonate U-9843, an HIV reverse transcriptase inhibitor
نویسندگان
چکیده
منابع مشابه
Balancing antiviral potency and host toxicity: identifying a nucleotide inhibitor with an optimal kinetic phenotype for HIV-1 reverse transcriptase.
Two novel thymidine analogs, 3'-fluoro-3'-deoxythymidine (FLT) and 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine (Ed4T), have been investigated as nucleoside reverse transcriptase inhibitors (NRTIs) for treatment of HIV infection. Ed4T seems very promising in phase II clinical trials, whereas toxicity halted FLT development during this phase. To understand these different molecular mechanisms of...
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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 ...
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Small RNA pseudoknots, selected to bind human immunodeficiency virus type 1 (HIV-1) reverse transcriptase tightly, are potent inhibitors of reverse transcriptase. The co-crystal structure of reverse transcriptase complexed with a 33 nucleotide RNA pseudoknot has been determined by fitting the ligand into a high quality, 4-fold averaged 4.8 A resolution electron density map. The RNA is kinked be...
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متن کاملHIV 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...
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ژورنال
عنوان ژورنال: Experientia
سال: 1994
ISSN: 0014-4754,1420-9071
DOI: 10.1007/bf01992044