Indolylarylsulfones, a fascinating story of highly potent human immunodeficiency virus type 1 non-nucleoside reverse transcriptase inhibitors [PDF]
Indolylarylsulfones are a potent class of human immunodeficiency virus type 1 non-nucleoside reverse transcriptase inhibitors. In this review, the structure activity relationship (SAR) studies to improve the profile of sulfone L-737,126 discovered by ...
Famiglini, V., Silvestri, R.
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BACKGROUND Human immunodeficiency virus type-1 (HIV-1) infection leads to acquired immunodeficiency syndrome (AIDS), a severe viral infection that has claimed approximately 658,507 lives in the US between the years 2010-2014. Antiretroviral (ARV) therapy
Ashley D Holec+3 more
semanticscholar +1 more source
Current scenario on non-nucleoside reverse transcriptase inhibitors (2018-present)
Acquired immune deficiency syndrome (AIDS) mainly caused by human immunodeficiency virus (HIV) type 1 (HIV-1) is a deadliest infectious disease, in which the immune system becomes ineffective and opportunistic infections accompany the disease.
Cui Deng+5 more
doaj
Treatment exhaustion of highly active antiretroviral therapy (HAART) among individuals infected with HIV in the United Kingdon: multicentre cohort study [PDF]
Objectives: To investigate whether there is evidence that an increasing proportion of HIV infected patients is starting to experience increases in viral load and decreases in CD4 cell count that are consistent with exhaustion of available treatment ...
Bhagani, S+13 more
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Discovery of non-nucleoside inhibitors of HIV-1 reverse transcriptase competing with the nucleotide substrate [PDF]
How odd! A new class of non-nucleoside reverse transcriptase inhibitors with a 6-vinylpyrimidine scaffold (1) has been found to inhibit HIV-1 reverse transcriptase (RT) by competition with the nucleotide substrate after binding to the non-nucleoside ...
Botta, Maurizio+10 more
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Selected Milestones in Antiviral Drug Development
This review article will describe the (wide) variety of approaches that I envisaged to develop a specific therapy for viral infections: (i) interferon and its inducers, (ii) HSV, VZV and CMV inhibitors, (iii) NRTIs (nucleoside reverse transcriptase ...
Erik De Clercq
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HIV-1 reverse transcriptase mutations that confer decreased in vitro susceptibility to anti-RT DNA aptamer RT1t49 confer cross resistance to other anti-RT aptamers but not to standard RT inhibitors [PDF]
RNA and DNA aptamers specific for HIV-1 reverse transcriptase (RT) can inhibit reverse transcription in vitro. RNA aptamers have been shown to potently block HIV-1 replication in culture.
Fisher, Timothy S+2 more
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Avoiding Drug Resistance in HIV Reverse Transcriptase.
HIV reverse transcriptase (RT) is an enzyme that plays a major role in the replication cycle of HIV and has been a key target of anti-HIV drug development efforts.
Maria E. Cilento+2 more
semanticscholar +1 more source
Adaptive HIV-1 evolutionary trajectories are constrained by protein stability [PDF]
Despite the use of combination antiretroviral drugs for the treatment of HIV-1 infection, the emergence of drug resistance remains a problem. Resistance may be conferred either by a single mutation or a concerted set of mutations.
Kandathil, Shaun M.+3 more
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TSAO compounds: The comprehensive story of a unique family of HIV-1 specific inhibitors of reverse transcriptase [PDF]
Emergence of drug-resistant viral strains is one of the major milestones and the main cause for the failure of antiretroviral therapy. Combination of different anti-HIV agents has E become the standard clinical practice to keep the viral load at low or ...
Balzarini, Jan+5 more
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