Results 31 to 40 of about 303,152 (296)

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

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   +1 more source

RNase HI Is Essential for Survival of Mycobacterium smegmatis. [PDF]

PLoS ONE, 2015
RNases H are involved in the removal of RNA from RNA/DNA hybrids. Type I RNases H are thought to recognize and cleave the RNA/DNA duplex when at least four ribonucleotides are present.
Alina E Minias, Anna M Brzostek, Malgorzata Korycka-Machala, Bozena Dziadek, Piotr Minias, Malini Rajagopalan, Murty Madiraju, Jaroslaw Dziadek   +7 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

Silencing Antibiotic Resistance with Antisense Oligonucleotides

Biomedicines, 2021
Antisense technologies consist of the utilization of oligonucleotides or oligonucleotide analogs to interfere with undesirable biological processes, commonly through inhibition of expression of selected genes.
Saumya Jani, Maria Soledad Ramirez, Marcelo E. Tolmasky   +2 more
doaj   +1 more source

From cycloheptathiophene-3-carboxamide to oxazinone-based derivatives as allosteric HIV-1 ribonuclease H inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
The paper focussed on a step-by-step structural modification of a cycloheptathiophene-3-carboxamide derivative recently identified by us as reverse transcriptase (RT)-associated ribonuclease H (RNase H) inhibitor.
Serena Massari, Angela Corona, Simona Distinto, Jenny Desantis, Alessia Caredda, Stefano Sabatini, Giuseppe Manfroni, Tommaso Felicetti, Violetta Cecchetti, Christophe Pannecouque, Elias Maccioni, Enzo Tramontano, Oriana Tabarrini   +12 more
doaj   +1 more source

Nonradioactive Detection of Retroviral- Associated RNase H Activity in a Microplate-Based, High-Throughput Format

BioTechniques, 2002
None of the available antiretroviral drugs that are currently used in the clinic to treat infection with HIV-1 is directed against the RNase H active site of the reverse transcriptase.
N. McLellan, X. Wei, B. Marchand, M.A. Wainberg, M. Götte   +4 more
doaj   +1 more source

Consecutive 5′- and 3′-amide linkages stabilise antisense oligonucleotides and elicit an efficient RNase H response

, 2020
Antisense oligonucleotides are now entering the clinic for hard-to-treat diseases. New chemical modifications are urgently required to enhance their drug-like properties.
Thorpe, Cameron, Epple, Sven, Baker, Ysobel, Brown, Tom, El-Sagheer, Afaf H   +4 more
core   +1 more source

Human immunodeficiency virus reverse transcriptase-associated RNase H activity

, 1989
Biochemical characteristics of the RNase H activity associated with immunoaffinity purified human immunodeficiency virus (HIV) reverse transcriptase (RT) were examined.
STARNES, M., CHENG, Y
core   +1 more source

Dimethyl fumarate combined with cisplatin at subcytotoxic doses sensitizes cervical cancer toward ferroptosis and apoptosis through GSH restriction and p53 (re)activation

Molecular Oncology, EarlyView.
Dimethyl fumarate (DMF) reduces growth of HPV‐positive cervical cancer spheroids and induces ferroptosis in cervical cancer cells via blocking SLC7A11/Glutathione (GSH) axis. Combination of subcytotoxic doses of DMF and cisplatin (CDDP) further suppresses spheroid growth and drives cell death in 2D culture models.
Carolina Punziano, Giuseppina Minopoli, Simona Romano, Laura Marrone, Katia Aquilano, Maria Lina Tornesello, Raffaella Faraonio   +6 more
wiley   +1 more source

The RNase J-Based RNA Degradosome Is Compartmentalized in the Gastric Pathogen Helicobacter pylori

mBio, 2020
Posttranscriptional regulation is a major level of gene expression control in any cell. In bacteria, multiprotein machines called RNA degradosomes are central for RNA processing and degradation, and some were reported to be compartmentalized inside these
Alejandro Tejada-Arranz, Eloïse Galtier, Lamya El Mortaji, Evelyne Turlin, Dmitry Ershov, Hilde De Reuse   +5 more
doaj   +1 more source