Avoiding drug resistance in HIV reverse transcriptase

ME Cilento, KA Kirby, SG Sarafianos - Chemical reviews, 2021 - ACS Publications
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. Because of the high …

Genotypic testing for human immunodeficiency virus type 1 drug resistance

RW Shafer - Clinical microbiology reviews, 2002 - Am Soc Microbiol
There are 16 approved human immunodeficiency virus type 1 (HIV-1) drugs belonging to
three mechanistic classes: protease inhibitors, nucleoside and nucleotide reverse …

[HTML][HTML] Mechanism-based approaches of 1, 3, 4 thiadiazole scaffolds as potent enzyme inhibitors for cytotoxicity and antiviral activity

D Kumar, H Kumar, V Kumar, A Deep, A Sharma… - Medicine in Drug …, 2023 - Elsevier
Significant progress in understanding cancer pathogenesis, it remains one of the leading
causes of death after cardiovascular diseases. Similarly viral infections have emerged from …

Therapeutic potential of uracil and its derivatives in countering pathogenic and physiological disorders

D Ramesh, BG Vijayakumar, T Kannan - European journal of medicinal …, 2020 - Elsevier
Uracil is one of the most notable pharmacophores in medicinal chemistry as the pyrimidine
nucleobase forms an integral part of many commercial drugs. Though the name uracil is …

Molecular basis of human immunodeficiency virus drug resistance: an update

L Menéndez-Arias - Antiviral research, 2010 - Elsevier
Antiretroviral therapy has led to a significant decrease in human immunodeficiency virus
(HIV)-related mortality. Approved antiretroviral drugs target different steps of the viral life …

Mechanisms of resistance to nucleoside analogue inhibitors of HIV-1 reverse transcriptase

L Menéndez-Arias - Virus research, 2008 - Elsevier
Human immunodeficiency virus (HIV) reverse transcriptase (RT) inhibitors can be classified
into nucleoside and nonnucleoside RT inhibitors. Nucleoside RT inhibitors are converted to …

Advances in nucleoside and nucleotide analogues in tackling human immunodeficiency virus and hepatitis virus infections

D Ramesh, BG Vijayakumar, T Kannan - ChemMedChem, 2021 - Wiley Online Library
Nucleoside and nucleotide analogues are structurally similar antimetabolites and are
promising small‐molecule chemotherapeutic agents against various infectious DNA and …

Structural basis of HIV-1 resistance to AZT by excision

X Tu, K Das, Q Han, JD Bauman, AD Clark Jr… - Nature structural & …, 2010 - nature.com
Abstract Human immunodeficiency virus (HIV-1) develops resistance to 3′-azido-2′, 3′-
deoxythymidine (AZT, zidovudine) by acquiring mutations in reverse transcriptase that …

HIV-1 reverse transcriptase and antiviral drug resistance. Part 2

K Das, E Arnold - Current opinion in virology, 2013 - Elsevier
Highlights•Discrimination and excision are major NRTI resistance mechanisms.•NRTIs used
in combination select different resistance mutations.•Complexes of NNRTI with RT-DNA in …

Thymidine analogue reverse transcriptase inhibitors resistance mutations profiles and association to other nucleoside reverse transcriptase inhibitors resistance …

AG Marcelin, C Delaugerre, M Wirden… - Journal of medical …, 2004 - Wiley Online Library
During ZDV or d4T exposure, mutations at codons 41, 67, 70, 210, 215, and 219 can be
selected and were named thymidine analogue mutations (TAMs). Some previous results …