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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 ...
Raymond Schinazi +2 more
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The majority of the drugs currently used for the treatment of HIV infections (AIDS) belong to either of the following three classes: nucleoside reverse transcriptase inhibitors (NRTIs), nonnucleoside reverse transcriptase inhibitors (NNRTIs), and protease inhibitors (PIs).
Erik De Clercq, De Clercq, Erik
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HIV resistance to reverse transcriptase inhibitors
Biochemical Pharmacology, 1994Erik de Clercq
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Investigational reverse transcriptase inhibitors for the treatment of HIV
INTRODUCTION: While considerable advances have been made in the development of antiretroviral agents, there is still work to be done. Reverse transcriptase inhibitors are important drugs for the treatment of HIV, and considerable research is currently ...
Santosh Kumar +2 more
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Reverse Transcriptase Inhibitors as Microbicides
Current HIV Research, 2012The CAPRISA 004 study in South Africa has accelerated the development of vaginal and rectal microbicides containing antiretrovirals that target specific enzymes in the reproduction cycle of HIV, especially reverse transcriptase inhibitors (RTI). In this review we discuss the potential relevance of HIV-1 RTIs as microbicides, focusing in the nucleotide ...
Lewi, P. +7 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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Mechanism of the action of the inhibitor of reverse transcriptase
Biochemical and Biophysical Research Communications, 1984An inhibitor of reverse transcriptase of Moloney leukemia virus was reported previously in the cytoplasm of the cultured cells (1). In this report, the mechanism of the inhibition was examined. The inhibitory activity was completely abrogated by treatment at 55 degrees C for 20 min.
M, Rokutanda, S T, Watanabe, Y Y, Maeda
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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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HIV Inhibitors Targeted at the Reverse Transcriptase
AIDS Research and Human Retroviruses, 1992HIV inhibitors targeted at the virus-associated reverse transcriptase (RT) can be divided into two groups, depending on whether they are targeted at the substrate or nonsubstrate binding site. To the first group belong the 2′,3′-dideoxynucleosides (i.e., DDC, DDI), 3′-azido-2′,3′-dideoxynucleosides (i.e., AZT), 3′-fluoro-2′,3 ...
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