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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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Pharmacokinetics of Reverse Transcriptase Inhibitors
2007The 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).
Patrick Hoggard +3 more
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Coumarins as Inhibitors of HIV Reverse Transcriptase
Current HIV Research, 2006Acquired 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).
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Quinolinehydrazones as inhibitors of retroviral reverse transcriptase.
Farmaco (Societa chimica italiana : 1989), 1992The inhibitory activity of a series of 2- and 4-quinolinehydrazones on retroviral reverse transcriptase has been studied on enzymes from M-MuLV, RAV-2, and on a crude lysate of HIV-1, assuming the first two enzymes as potential models of the third. The highest activity is mainly found in lipophilic, water soluble 4-quinolinehydrazones.
C. Bartolucci +7 more
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Trends in kinase drug discovery: targets, indications and inhibitor design
Nature Reviews Drug Discovery, 2021Misty M Attwood, Stefan Knapp
exaly