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HIV nucleoside reverse transcriptase inhibitors
European Journal of Medicinal Chemistry, 2022More than 40 years into the pandemic, HIV remains a global burden and as of now, there is no cure in sight. Fortunately, highly active antiretroviral therapy (HAART) has been developed to manage and suppress HIV infection. Combinations of two to three drugs targeting key viral proteins, including compounds inhibiting HIV reverse transcriptase (RT ...
Franck, Amblard +8 more
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Nonnucleoside reverse transcriptase inhibitors
Drugs of the Future, 2000The non-nucleoside reverse transcriptase inhibitors (NNRTIs) directly inhibit the HIV-1 reverse transcriptase (RT) by binding in a reversible and non-competitive manner to the enzyme. The currently available NNRTIs are nevirapine, delavirdine, and efavirenz; other compounds are under evaluation.
null Hajos, G. +3 more
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HIV-1 reverse transcriptase inhibitors
Applied Microbiology and Biotechnology, 2007Reverse transcriptase (RT) is one of the three enzymes encoded by the human immunodeficiency virus type 1 (HIV-1), the etiological agent of AIDS. Together with protease inhibitors, drugs inhibiting the RNA- and DNA-dependant DNA polymerase activity of RT are the major components of highly active antiretroviral therapy (HAART), which has dramatically ...
El Safadi, Yazan +2 more
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Hepatotoxicity of Nucleoside Reverse Transcriptase Inhibitors
Seminars in Liver Disease, 2003Hepatotoxicity is an adverse effect of all available classes of antiretrovirals, including nucleoside reverse transcriptase inhibitors (NRTI). A syndrome of hepatic steatosis and lactic acidosis has been recognized as a rare, potentially fatal complication since the advent of NRTI monotherapy in the early 1990s.
Valentina, Montessori +2 more
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New Reverse Transcriptase Inhibitors
1999Reverse transcriptase inhibitors used in the treatment of HIV-1 infection include the nucleoside analogues zidovudine, didanosine, zalcitabine, lamivudine and stavudine. More recently a number of other classes of reverse transcriptase inhibitors have been discovered, and are in various phases of clinical trial. This chapter will focus on the nucleoside
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AIDS, 2009
The use of nonnucleoside reverse transcriptase inhibitor (NNRTI) + protease inhibitor regimen for the treatment of antiretroviral-naive patients was less successful than classical nucleoside reverse transcriptase inhibitor (NRTI) based regimen and associated with more resistance for protease inhibitors and NNRTIs. The selection for NNRTI resistance was
Cathia, Soulié +10 more
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The use of nonnucleoside reverse transcriptase inhibitor (NNRTI) + protease inhibitor regimen for the treatment of antiretroviral-naive patients was less successful than classical nucleoside reverse transcriptase inhibitor (NRTI) based regimen and associated with more resistance for protease inhibitors and NNRTIs. The selection for NNRTI resistance was
Cathia, Soulié +10 more
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Inhibitors of HIV‐1 Reverse Transcriptase
2008Publisher Summary With the identification of human immunodeficiency virus (HIV)‐1 as the infectious agent leading to acquired immune deficiency syndrome (AIDS), the viral reverse transcriptase (RT) has been a primary focus for drug discovery and development. Currently, two classes of RT inhibitors are used clinically. Nucleoside reverse transcriptase
Tatiana, Ilina, Michael A, Parniak
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Novel HIV-1 reverse transcriptase inhibitors
Virus Research, 2008HIV-1 reverse transcriptase (RT) was the first viral enzyme to be targeted by anti-HIV drugs. Despite 20 years of experience with RT inhibitors, new ways to inhibit this target and address viral resistance continue to emerge. In both licensed RT inhibitor classes, nucleosides (NRTIs) and non-nucleosides (NNRTIs), compounds with better resistance ...
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Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs)
2013HIV is a retrovirus; the retroviral life cycle is characterized by two specific steps: (1) the conversion of the single-stranded RNA genome found in the virion into double-stranded DNA by the viral enzyme reverse transcriptase (RT) and (2) the subsequent insertion of this DNA copy into the host genome by the viral enzyme integrase.
Kalyan Das +2 more
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[Reverse transcriptase inhibitors, protease inhibitors].
Nihon rinsho. Japanese journal of clinical medicine, 2012These are six different classes of antiretroviral drugs that are nucleoside/nucleotide reverse transcriptase inhibitors(NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), fusion inhibitors, CCR5 inhibitors and integrase inhibitors. NRTIs are thought as backbone of HAART(highly active antiretroviral therapy) and
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