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

L Battini, M Bollini - Medicinal Research Reviews, 2019 - Wiley Online Library
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. Highly active …

[HTML][HTML] Targeting HIV-1 Reverse transcriptase using a fragment-based approach

M Mansouri, S Rumrill, S Dawson, A Johnson… - Molecules, 2023 - mdpi.com
Human immunodeficiency virus type I (HIV-1) is a retrovirus that infects cells of the host's
immune system leading to acquired immunodeficiency syndrome and potentially death …

Advances in the development of pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors

H Vite-Caritino, O Méndez-Lucio, H Reyes, A Cabrera… - RSC …, 2016 - pubs.rsc.org
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are part of a structurally diverse
family with distinct features attractive for the treatment of AIDS that continues to be a major …

[HTML][HTML] Targeting the Structural Maturation Pathway of HIV-1 Reverse Transcriptase

TW Kirby, SA Gabel, EF DeRose, L Perera, JM Krahn… - Biomolecules, 2023 - mdpi.com
Formation of active HIV-1 reverse transcriptase (RT) proceeds via a structural maturation
process that involves subdomain rearrangements and formation of an asymmetric …

Application of site‐specific spin labeling for NMR detecting inhibitor‐induced conformational change of HIV‐1 reverse transcriptase

S Seetaha, M Yagi‐Utsumi, T Yamaguchi… - …, 2016 - Wiley Online Library
Paramagnetism‐assisted nuclear magnetic resonance (NMR) techniques can provide long‐
range structural information complemented with local information derived from chemical …

[HTML][HTML] The structure of FIV reverse transcriptase and its implications for non-nucleoside inhibitor resistance

M Galilee, A Alian - PLoS pathogens, 2018 - journals.plos.org
Reverse transcriptase (RT) is the target for the majority of anti-HIV-1 drugs. As with all anti-
AIDS treatments, continued success of RT inhibitors is persistently disrupted by the …

Structure-based virtual screening efforts against HIV-1 reverse transcriptase to introduce the new potent non-nucleoside reverse transcriptase inhibitor

Y Hosseini, A Mollica, S Mirzaie - Journal of Molecular Structure, 2016 - Elsevier
The human immunodeficiency virus (HIV) which is strictly related to the development of
AIDS, is treated by a cocktail of drugs, but due its high propensity gain drug resistance, the …

Biophysical Characterization of p51 and p66 Monomers of HIV-1 Reverse Transcriptase with Their Inhibitors

S Seetaha, N Kamonsutthipaijit, M Yagi-Utsumi… - The Protein …, 2023 - Springer
Abstract Human immunodeficiency virus (HIV)-1 reverse transcriptase (HIV-1 RT) is
responsible for the transcription of viral RNA genomes into DNA genomes and has become …

[HTML][HTML] Large Multidomain Protein NMR: HIV-1 Reverse Transcriptase Precursor in Solution

TV Ilina, Z Xi, T Brosenitsch, N Sluis-Cremer… - International Journal of …, 2020 - mdpi.com
NMR studies of large proteins, over 100 kDa, in solution are technically challenging and,
therefore, of considerable interest in the biophysics field. The challenge arises because the …

[HTML][HTML] Biophysical characterization of novel DNA aptamers against K103N/Y181C double mutant HIV-1 reverse transcriptase

S Ratanabunyong, S Seetaha, S Hannongbua… - Molecules, 2022 - mdpi.com
The human immunodeficiency virus type-1 Reverse Transcriptase (HIV-1 RT) plays a pivotal
role in essential viral replication and is the main target for antiviral therapy. The anti-HIV-1 …