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Hepatotoxicity of Nucleoside Reverse Transcriptase Inhibitors

Seminars in Liver Disease, 2003
Hepatotoxicity 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
openaire   +3 more sources

Current and emerging non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV-1 treatment

Expert Opinion on Drug Metabolism & Toxicology, 2019
Introduction: Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are essential components of highly active antiretroviral therapy against HIV-1 infections. Here, we provide a comprehensive overview of approved and emerging NNRTIs.
Yali Wang, E. De Clercq, Guangdi Li
semanticscholar   +1 more source

Challenges and approaches in the discovery of human immunodeficiency virus type‐1 non‐nucleoside reverse transcriptase inhibitors

Medicinal research reviews (Print), 2018
The type I human immunodeficiency virus (HIV‐1) pandemic affecting over 37 million people worldwide continues, with 1.8 million people newly infected each year.
Leandro Battini, Mariela Bollini
semanticscholar   +1 more source

New Reverse Transcriptase Inhibitors [PDF]

open access: possible, 1999
Reverse 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
openaire   +2 more sources

Mechanism of the action of the inhibitor of reverse transcriptase

Biochemical and Biophysical Research Communications, 1984
An 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.
Yukiko Y. Maeda   +2 more
openaire   +3 more sources

Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.

Journal of Medicinal Chemistry, 2016
We designed and synthesized a series of human immunodeficiency virus type 1 (HIV-1) non-nucleoside reverse transcriptase inhibitors (NNRTIs) with a piperidine-substituted thiophene[3,2-d]pyrimidine scaffold, employing a strategy of structure-based ...
Dongwei Kang   +13 more
semanticscholar   +1 more source

Pharmacokinetics of Reverse Transcriptase Inhibitors

2007
The nucleoside reverse transcriptase inhibitors (NRTIs) were the first class of compounds discovered to be potent inhibitors of HIV replication (1 and, to date, these drugs remain the backbone of antiretroviral therapy. NRTIs are essentially prodrugs, inactive in their parent form and requiring activation to exert their antiviral effects (2, 3).
Stephen Kewn   +3 more
openaire   +2 more sources

Inhibitors of HIV‐1 Reverse Transcriptase

2008
Publisher 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 V Ilina, Michael A. Parniak
openaire   +3 more sources

Coumarins as Inhibitors of HIV Reverse Transcriptase

Current HIV Research, 2006
Acquired immunodeficiency syndrome (AIDS), a degenerative disease of the immune and central nervous systems, is an enormous world-wide health threat. No cure has been found, and research is aimed at developing chemotherapy against the causative agent, human immunodeficiency virus (HIV).
openaire   +3 more sources

Interruption of reverse transcriptase inhibitors or a switch from reverse transcriptase to protease inhibitors resulted in a fast reappearance of virus strains with a reverse transcriptase inhibitor-sensitive genotype

AIDS, 1999
To study the effect of the interruption of reverse transriptase inhibitor (RTI) therapy or a switch from RTI to protease inhibitors, on the genotypic drug-resistance pattern of plasma HIV-1.Nine patients who completely stopped all medication, and five patients who switched from a treatment with RTI to a regimen containing protease inhibitors only, were
Beatrijs Van Der Gucht   +4 more
openaire   +2 more sources

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