Antisense Research and Application

doi:10.1007/978-3-642-58785-6

Cited by 36 publications

(1 citation statement)

References 561 publications

(863 reference statements)

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“…The replacement of oxygen by sulfur is a powerful strategy employed by medicinal chemists to improve biophysical properties of phosphate containing molecules. This so-called “thio effect” has proven to be clinically validated in the case of oligonucleotide therapeutics by improving cellular uptake and stability toward enzymatic degradation in the extracellular medium (Figure A, left). − Although this strategy proved to be highly advantageous in the field of oligonucleotides, single-atom replacement on the phosphate backbone is underexplored in other areas of medicinal chemistry. Previous research has shown that phosphonates can act as mimics for other functional groups i.e.…”

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confidence: 99%

Stereocontrolled Radical Thiophosphorylation

et al. 2023

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The first practical, fully stereoselective P(V)-radical hydrophosphorylation is presented herein by using simple, limonene-derived reagent systems. A set of reagents have been developed that upon radical initiation react smoothly with olefins and other radical acceptors to generate P-chiral products, which can be further diversified (with conventional 2e– chemistry) to a range of underexplored bioisosteric building blocks. The reactions have a wide scope with excellent chemoselectivity, and the unexpected stereochemical outcome has been supported computationally and experimentally. Initial ADME studies are suggestive of the promising properties of this rarely explored chemical space.

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confidence: 99%

Stereocontrolled Radical Thiophosphorylation

et al. 2023

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Prooligonucleotide metabolism in a crude cell extract followed by matrix-assisted laser desorption/ionisation time-of-flight mass spectrometry

Lioux

Lefèbvre

Vasseur

et al. 1999

Rapid Commun. Mass Spectrom.

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Oligonucleotide Therapeutics

Crooke¹

2003

Burger's Medicinal Chemistry and Drug Discovery

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Antisense technology expolits oligonucleotide analogs to bind to cognate RNA sequences through Watson‐Crick hybridization resulting in the destruction or disablement of the target RNA. Durign the past decade, programs on all fronts has continued and there are satisfactory consensus to all the basic questions. In this review, progress in the medicinal chemistry and molecular pharmacology of antisense is reviewed. Further, progress in understanding thepharmacokinetic, pharmacodynamic and toxicologic properties of first and second generations antisense drugs is reviewed. Additionally, a summary of clinical data on a significant number of antisense drugs is provided.

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Antisense Research and Application

Cited by 36 publications

References 561 publications

Stereocontrolled Radical Thiophosphorylation

Stereocontrolled Radical Thiophosphorylation

Prooligonucleotide metabolism in a crude cell extract followed by matrix-assisted laser desorption/ionisation time-of-flight mass spectrometry

Oligonucleotide Therapeutics

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