HIV-1 Protease Inhibitors

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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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Screening Efficacy of Available HIV Protease Inhibitors on COVID-19 Protease

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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HIV protease inhibitors and atherosclerosis.

The advent of highly active antiretroviral therapy (HAART), including the use of HIV protease inhibitors (PIs) has significantly reduced the morbidity and mortality of AIDS in HIV infected patients. Unfortunately, the adverse effects of PIs, including dyslipidemia, lipodystrophy, insulin resistance, and premature atherosclerosis, are cause for concern for their use in chronic management of HIV ...

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Lipopeptides as dimerization inhibitors of HIV-1 protease.

In AIDS therapy, attempts have been made to inhibit the virus-encoded enzymes, e.g. HIV-1 protease, using active site-directed inhibitors. This approach is questionable, however, due to virus mutations and the high toxicity of the drugs. An alternative method to inhibit the dimeric HIV protease is the targeting of the interface region of the protease subunits in order to prevent subunit dimeriz...

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Approaches to the design of effective HIV-1 protease inhibitors.

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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ژورنال

عنوان ژورنال: Clinical Infectious Diseases

سال: 2000

ISSN: 1537-6591,1058-4838

DOI: 10.1086/313853