Identification of HIV-1 Reverse Transcriptase-Associated Ribonuclease H Inhibitors Based on 2-Hydroxy-1,4-naphthoquinone Mannich Bases [PDF]
MoleculesThere is a strong demand for new and efficient antiviral compounds. A series of 2-hydroxy-1,4-naphthoquinone Mannich bases were screened for their HIV-1-RNase H inhibitory activity.
Nhat Quang Tu +9 more
doaj +3 more sources
Discovery of Benzisothiazolone Derivatives as Bifunctional Inhibitors of HIV-1 Reverse Transcriptase DNA Polymerase and Ribonuclease H Activities [PDF]
BiomoleculesThe ribonuclease H (RNase H) active site of HIV-1 reverse transcriptase (RT) is the only viral enzyme not targeted by approved antiretroviral drugs. Using a fluorescence-based in vitro assay, we screened 65,239 compounds at a final concentration of 10 µM
Alondra Vázquez Rivera +7 more
doaj +6 more sources
Thermal adaptation of conformational dynamics in ribonuclease H. [PDF]
PLoS Computational Biology, 2013 The relationship between inherent internal conformational processes and enzymatic activity or thermodynamic stability of proteins has proven difficult to characterize. The study of homologous proteins with differing thermostabilities offers an especially
Kate A Stafford +2 more
doaj +4 more sources
The hepatitis B virus ribonuclease H is sensitive to inhibitors of the human immunodeficiency virus ribonuclease H and integrase enzymes. [PDF]
PLoS Pathogens, 2013 Nucleos(t)ide analog therapy blocks DNA synthesis by the hepatitis B virus (HBV) reverse transcriptase and can control the infection, but treatment is life-long and has high costs and unpredictable long-term side effects.
John E Tavis +10 more
doaj +4 more sources
Inhibitors of HIV-1 Reverse Transcriptase—Associated Ribonuclease H Activity [PDF]
Biology, 2012 HIV-1 enzyme reverse transcriptase (RT) is a major target for antiviral drug development, with over half of current FDA-approved therapeutics against HIV infection targeting the DNA polymerase activity of this enzyme. HIV-1 RT is a multifunctional enzyme
Michael A. Parniak +4 more
doaj +4 more sources
The catalytic mechanism, metal dependence, substrate specificity, and biodiversity of ribonuclease H [PDF]
Frontiers in Microbiology, 2022 Ribonucleoside monophosphates are inevitably misincorporated into the DNA genome inside cells, and they need to be excised to avoid chromosome instability.
Jing Pang, Qinyu Guo, Zheng Lu
doaj +2 more sources
Analogs of the Catechol Derivative Dynasore Inhibit HIV-1 Ribonuclease H, SARS-CoV-2 nsp14 Exoribonuclease, and Virus Replication [PDF]
Viruses, 2023 Viral replication often depends on RNA maturation and degradation processes catalyzed by viral ribonucleases, which are therefore candidate targets for antiviral drugs.
Abhishek Asthana +10 more
doaj +2 more sources
Evolution of ribonuclease H genes in prokaryotes to avoid inheritance of redundant genes [PDF]
BMC Evolutionary Biology, 2007 Background A theoretical model of genetic redundancy has proposed that the fates of redundant genes depend on the degree of functional redundancy, and that functionally redundant genes will not be inherited together.
Tomita Masaru +2 more
doaj +2 more sources
Discovery of bimodal hepatitis B virus ribonuclease H and capsid assembly inhibitors. [PDF]
PLoS PathogensHepatitis B virus (HBV) ribonuclease H (RNaseH) inhibitors are a potent class of antivirals that prevent degradation of the viral pregenomic RNA during reverse transcription and block formation of mature HBV DNAs.
Daniel P Bradley +9 more
doaj +2 more sources
1,2,4-Triazolo[1,5-a]pyrimidines as a Novel Class of Inhibitors of the HIV-1 Reverse Transcriptase-Associated Ribonuclease H Activity [PDF]
Molecules, 2020 Despite great efforts have been made in the prevention and therapy of human immunodeficiency virus (HIV-1) infection, however the difficulty to eradicate latent viral reservoirs together with the emergence of multi-drug-resistant strains require the ...
Jenny Desantis +10 more
doaj +2 more sources