Adaptive inhibitors of the HIV-1 protease
نویسندگان
چکیده
منابع مشابه
HIV-1 protease inhibitors.
Treatment of human immunodeficiency virus type 1 (HIV-1) infection with regimens that include protease inhibitors (PIs) has contributed to marked improvements in HIV-related disease progression and mortality. Five PIs are approved by the US Food and Drug Administration and have potent activity in vitro. PIs with 2 nucleoside analogue reverse transcriptase inhibitors have demonstrated prolonged ...
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Background and Aim: Advent of COVID-19 attracted the attentions of researchers to develop drugs for its treatment. Besides efforts on developing new drugs, screening available drugs for efficacy on COVID-19 could be an urgent action of initiating its pharmacotherapy. In this study, efficacy of HIV protease inhibitors on COVID-19 protease has been examined. Methods: Molecular docking based scree...
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Recently, western countries have recorded a decrease in the death rate imputed to AIDS. This success has been largely attributed to the presence on the market of chemotherapies that inhibit the infectivity of the predominant causative agent, the HIV-1 virus, by targeting essential viral enzymes. One of these is the protease (HIV-1 PR) whose activity is a prerequisite for viral replication. Two ...
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The development of HIV-1 protease inhibitors (HPIs) in highly active antiretroviral therapy (HAART) has dramatically decreased AIDS mortality. However, HPIs exhibit suboptimal therapeutics in vivo due to their intrinsic low oral absorption and rapid efflux via ATP-binding cassette transporters. These attributes facilitate uninhibited viral propagation and rapid selection of drug resistant HIV-1...
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Defective variants of human immunodeficiency virus type 1 (HIV-1) protease (HIV PR) have been engineered to inhibit wild-type (wt) HIV PR activity. These variants were designed to promote the formation of heterodimers and to destabilize the formation of inactive variant homodimers of HIV-1 protease through substitutions at Asp-25, Ile-49, and Gly-50 (Babé, L. M., Rosé, J., and Craik, C. S. (199...
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ژورنال
عنوان ژورنال: Progress in Biophysics and Molecular Biology
سال: 2005
ISSN: 0079-6107
DOI: 10.1016/j.pbiomolbio.2004.07.005