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Update on Recent Developments in Small Molecular HIV-1 RNase H Inhibitors (2013-2016): Opportunities and Challenges.

Current Medicinal Chemistry, 2018
Combinations of antiretroviral drugs are successfully used to treat HIV-infected patients. However, drug resistance is a major problem that makes discovery of new antiretroviral drugs an ongoing priority.
Xueshun Wang   +4 more
semanticscholar   +1 more source

Stereochemical Course of Escherichia coli RNase H.

ChemInform, 2002
A new enzymatic method has allowed the assignment of the stereochemistry of E. coli RNase-H-assisted hydrolysis of RNA labelled within the scissile bond with (R(p))-phosphorothioate. This method is based on a stereospecific, two-step enzymatic conversion of cytidine 5'-[(18)O]phosphorothioate into the corresponding 5'-alpha-[(18)O]thiotriphosphate ...
Alina Owczarek   +3 more
openaire   +4 more sources

Pyridopyrimidinone inhibitors of HIV-1 RNase H

European Journal of Medicinal Chemistry, 2014
Using a structure based pharmacophore design, a weak inhibitor of RNase H, identified from a small library of two metal binding HIV-1 integrase inhibitors, was optimized for potency and physicochemical properties. This manuscript describes the SAR and in vivo DMPK for the pyridopyrimidinone class of inhibitors.
Emile J. Velthuisen   +11 more
openaire   +3 more sources

An enzyme-initiated DNAzyme motor for RNase H activity imaging in living cell.

Chemical Communications, 2019
In this work, we have developed a novel DNAzyme motor initiated by endogenous enzyme for sensitive imaging of intracellular RNase H activity.
Namin Hu   +9 more
semanticscholar   +1 more source

RNase H Activation by Stereoregular Boranophosphate Oligonucleotide

ChemInform, 2003
AbstractFor Abstract see ChemInform Abstract in Full Text.
Dmitri S. Sergueev   +3 more
openaire   +4 more sources

The RNase H Mechanism

2007
Antisense oligonucleotides (ASOs) are designed to modulate the information transfer from gene to protein-in essence to alter mRNA intermediary metabolism. mRNA intermediary metabolism is extremely complex beginning with transcription and concluding with degradation usually after translation.
Hongjiang Wu   +2 more
openaire   +2 more sources

A radar-like DNA monitor for RNase H-targeted natural compounds screening and RNase H activity in situ detection

The Analyst, 2021
Radar-like monitor for RNase H detection in vitro and for intercellular imaging.
Yalei Hu   +6 more
openaire   +3 more sources

CHAPTER 3. The Medicinal Chemistry of RNase H-activating Antisense Oligonucleotides

Drug Discovery, 2019
This review focuses on the properties that an RNase H-activating antisense oligonucleotide (ASO) drug must have to function effectively in animals, as well as on medicinal chemistry strategies to achieve these properties.
P. Seth, E. Swayze
semanticscholar   +1 more source

A label-free and enzyme-free signal amplification strategy for a sensitive RNase H activity assay.

Nanoscale, 2017
We herein describe a label-free and enzyme-free signal amplification strategy for the sensitive determination of ribonuclease H (RNase H) activity, which relies on the target-triggered catalytic hairpin assembly (CHA) in conjunction with a G-quadruplex ...
C. Lee, Hyowon Jang, K. S. Park, H. Park
semanticscholar   +1 more source

Boranophosphates Support the RNase H Cleavage of Polyribonucleotides

Antisense and Nucleic Acid Drug Development, 1999
Modification of the phosphodiester linkages in DNA by replacing one of the nonbridging oxygens with borane, BH3, produces an isoelectronic mimic of DNA called boranophosphates. Nonstereoregular oligodeoxyribonucleoside all-boranophosphates are shown here for the first time to elicit the RNase H hydrolysis of polyribonucleotides. We compared the ability
Vladimir Rait, Barbara Ramsay Shaw
openaire   +2 more sources

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