HIV-1 antiretroviral resistance: scientific principles and clinical applications

MW Tang, RW Shafer - Drugs, 2012 - Springer
The efficacy of an antiretroviral (ARV) treatment regimen depends on the activity of the
regimen's individual ARV drugs and the number of HIV-1 mutations required for the …

Antiretroviral treatment of HIV-2 infection: available drugs, resistance pathways, and promising new compounds

I Moranguinho, N Taveira, I Bártolo - International Journal of Molecular …, 2023 - mdpi.com
Currently, it is estimated that 1–2 million people worldwide are infected with HIV-2,
accounting for 3–5% of the global burden of HIV. The course of HIV-2 infection is longer …

Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms

D Li, P Zhan, E De Clercq, X Liu - Journal of medicinal chemistry, 2012 - ACS Publications
Currently, five NNRTIs have been approved by US Food and Drug Administration (US FDA)
for the clinical treatment of AIDS, ie, nevirapine, delavirdine, efavirenz, etravirine, and …

Structural basis of HIV inhibition by translocation-defective RT inhibitor 4′-ethynyl-2-fluoro-2′-deoxyadenosine (EFdA)

ZL Salie, KA Kirby, E Michailidis… - Proceedings of the …, 2016 - National Acad Sciences
4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) is the most potent nucleoside analog
inhibitor of HIV reverse transcriptase (RT). It retains a 3′-OH yet acts as a chain-terminating …

Internal RNA 2′-O-methylation on the HIV-1 genome impairs reverse transcription

A Decombe, O Peersen, P Sutto-Ortiz… - Nucleic Acids …, 2024 - academic.oup.com
Viral RNA genomes are modified by epitranscriptomic marks, including 2′-O-methylation
that is added by cellular or viral methyltransferases. 2′-O-Methylation modulates RNA …

A structural view on medicinal chemistry strategies against drug resistance

S Agnello, M Brand, MF Chellat… - Angewandte Chemie …, 2019 - Wiley Online Library
The natural phenomenon of drug resistance is a widespread issue that hampers the
performance of drugs in many major clinical indications. Antibacterial and antifungal drugs …

Effect of mutations at position E138 in HIV-1 reverse transcriptase and their interactions with the M184I mutation on defining patterns of resistance to nonnucleoside …

HT Xu, SP Colby-Germinario… - Antimicrobial agents …, 2013 - Am Soc Microbiol
Impacts of mutations at position E138 (A/G/K/Q/R/V) alone or in combination with M184I in
HIV-1 reverse transcriptase (RT) were investigated. We also determined why E138K is the …

[HTML][HTML] Chemical characterization, antioxidant and anti-HIV activities of a Brazilian propolis from Ceará state

CCF Silva, A Salatino, LB Motta, G Negri… - Revista Brasileira de …, 2019 - SciELO Brasil
Propolis (bee glue) a product of Apis mellifera L. is a resinous mixture containing chiefly
beeswax and resin harvested by bees from plant leaves, buds and exudates. Extracts of a …

HIV-1 RT-associated RNase H function inhibitors: recent advances in drug development

E Tramontano, R Di Santo - Current medicinal chemistry, 2010 - ingentaconnect.com
The HIV-1 genomic RNA reverse transcription is an essential step in the virus cycle carried
out by the viral-coded reverse transcriptase (RT), which has two associated functions: the …

Biochemical mechanism of HIV-1 resistance to rilpivirine

K Singh, B Marchand, DK Rai, B Sharma… - Journal of Biological …, 2012 - ASBMB
Rilpivirine (RPV) is a second generation nonnucleoside reverse transcriptase (RT) inhibitor
(NNRTI) that efficiently inhibits HIV-1 resistant to first generation NNRTIs. Virological failure …