Results 11 to 20 of about 61,817 (251)

Discovery of Benzisothiazolone Derivatives as Bifunctional Inhibitors of HIV-1 Reverse Transcriptase DNA Polymerase and Ribonuclease H Activities [PDF]

Biomolecules
The 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, Heather Donald, Mounia Alaoui-El-Azher, John J. Skoko, John S. Lazo, Michael A. Parniak, Paul A. Johnston, Nicolas Sluis-Cremer   +7 more
doaj   +2 more sources

Scaffold hopping and optimisation of 3’,4’-dihydroxyphenyl- containing thienopyrimidinones: synthesis of quinazolinone derivatives as novel allosteric inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Bioisosteric replacement and scaffold hopping are powerful strategies in drug design useful for rationally modifying a hit compound towards novel lead therapeutic agents.
Graziella Tocco, Francesca Esposito, Pierluigi Caboni, Antonio Laus, John A. Beutler, Jennifer A. Wilson, Angela Corona, Stuart F. J. Le Grice, Enzo Tramontano   +8 more
doaj   +2 more sources

The hepatitis B virus ribonuclease H as a drug target [PDF]

Antiviral Research, 2015
Chronic hepatitis B virus (HBV) infection is a leading cause of hepatitis, liver failure, and hepatocellular carcinoma. An outstanding vaccine is available; however, the number of infections remains high. Current anti-HBV treatments with interferon α and nucleos(t)ide analogs clear the infection in only a small minority of patients, and either induce ...
John E, Tavis, Elena, Lomonosova
openaire   +3 more sources

Convergent Evolution of Ribonuclease H in LTR Retrotransposons and Retroviruses [PDF]

Molecular Biology and Evolution, 2015
Ty3/Gypsy long terminals repeat (LTR) retrotransposons are structurally and phylogenetically close to retroviruses. Two notable structural differences between these groups of genetic elements are 1) the presence in retroviruses of an additional envelope gene, env, which mediates infection, and 2) a specific dual ribonuclease H (RNH) domain encoded by ...
Ustyantsev, Kirill, Novikova, Olga, Blinov, Alexander, Smyshlyaev, Georgy   +3 more
openaire   +3 more sources

Ribonuclease H: the enzymes in eukaryotes [PDF]

The FEBS Journal, 2009
Ribonucleases H are enzymes that cleave the RNA of RNA/DNA hybrids that form during replication and repair and which could lead to DNA instability if they were not processed. There are two main types of RNase H, and at least one of them is present in most organisms.
Susana M, Cerritelli, Robert J, Crouch
openaire   +2 more sources

Acetylation regulates the oligomerization state and activity of RNase J, the Helicobacter pylori major ribonuclease

Nature Communications, 2023
In the gastric pathogen Helicobacter pylori, post-transcriptional regulation relies strongly on the activity of the essential ribonuclease RNase J. Here, we elucidated the crystal and cryo-EM structures of RNase J and determined that it assembles into ...
Alejandro Tejada-Arranz, Aleksei Lulla, Maxime Bouilloux-Lafont, Evelyne Turlin, Xue-Yuan Pei, Thibaut Douché, Mariette Matondo, Allison H. Williams, Bertrand Raynal, Ben F. Luisi, Hilde De Reuse   +10 more
doaj   +1 more source

Production of ovine Pancreatic Ribonuclease and investigation of enzyme characteristics [PDF]

پژوهشهای علوم دامی ایران, 2021
Introduction Obviously, the recent decades strategy in cancer therapy, anticancer drug discovery and drug improvement is to characterize, distinguish and validate the most promising cancer-related molecular targets to which new drugs can be designed. The
mahsa Zabetian, Mohammad reza Nasiri, Ali Javadmannesh, Shahrokh ghovati   +3 more
doaj   +1 more source

Inhibitors of HIV-1 Reverse Transcriptase—Associated Ribonuclease H Activity

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, Stefan G. Sarafianos, Rieko Ishima, Krystal LaBarge, Tatiana Ilina   +4 more
doaj   +1 more source

Exploring New Scaffolds for the Dual Inhibition of HIV-1 RT Polymerase and Ribonuclease Associated Functions

Molecules, 2021
Current therapeutic protocols for the treatment of HIV infection consist of the combination of diverse anti-retroviral drugs in order to reduce the selection of resistant mutants and to allow for the use of lower doses of each single agent to reduce ...
Rita Meleddu, Angela Corona, Simona Distinto, Filippo Cottiglia, Serenella Deplano, Lisa Sequeira, Daniela Secci, Alessia Onali, Erica Sanna, Francesca Esposito, Italo Cirone, Francesco Ortuso, Stefano Alcaro, Enzo Tramontano, Péter Mátyus, Elias Maccioni   +15 more
doaj   +1 more source

HIV-1 Ribonuclease H: Structure, Catalytic Mechanism and Inhibitors

Viruses, 2010
Since the human immunodeficiency virus (HIV) was discovered as the etiological agent of acquired immunodeficiency syndrome (AIDS), it has encouraged much research into antiviral compounds.
Greg L. Beilhartz, Matthias Götte
doaj   +1 more source