Impact of Phosphorothioate Chirality on Double‐Stranded siRNAs: A Systematic Evaluation of Stereopure siRNA Designs

The current state and future directions of RNAi-based therapeutics

(2019) Ryan L. Setten et al.   NATURE REVIEWS DRUG DISCOVERY

Novel Cluster and Monomer-Based GalNAc Structures Induce Effective Uptake of siRNAs in Vitro and in Vivo

(2018) Vivek K. Sharma et al.   BIOCONJUGATE CHEMISTRY

Unlocking P(V): Reagents for chiral phosphorothioate synthesis

(2018) Kyle W. Knouse et al.   SCIENCE

Control of phosphorothioate stereochemistry substantially increases the efficacy of antisense oligonucleotides

(2017) Naoki Iwamoto et al.   NATURE BIOTECHNOLOGY

Therapeutic miRNA and siRNA: Moving from Bench to Clinic as Next Generation Medicine

(2017) Chiranjib Chakraborty et al.   Molecular Therapy-Nucleic Acids

siRNA Delivery Strategies: A Comprehensive Review of Recent Developments

(2017) Katyayani Tatiparti et al.   Nanomaterials

Well-Defined Multivalent Ligands for Hepatocytes Targeting via Asialoglycoprotein Receptor

(2016) Xiangang Huang et al.   BIOCONJUGATE CHEMISTRY

Precise and efficient siRNA design: a key point in competent gene silencing

(2016) E Fakhr et al.   CANCER GENE THERAPY

The Medicinal Chemistry of Therapeutic Oligonucleotides

(2016) W. Brad Wan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Stabilin-1 and Stabilin-2 are specific receptors for the cellular internalization of phosphorothioate-modified antisense oligonucleotides (ASOs) in the liver

(2016) Colton M. Miller et al.   NUCLEIC ACIDS RESEARCH

Phosphorothioate backbone modifications of nucleotide-based drugs are potent platelet activators

(2015) Ulrike Flierl et al.   JOURNAL OF EXPERIMENTAL MEDICINE

An RNAi therapeutic targeting antithrombin to rebalance the coagulation system and promote hemostasis in hemophilia

(2015) Alfica Sehgal et al.   NATURE MEDICINE

2′-Fluoro-modified phosphorothioate oligonucleotide can cause rapid degradation of P54nrb and PSF

(2015) Wen Shen et al.   NUCLEIC ACIDS RESEARCH

Stereochemical bias introduced during RNA synthesis modulates the activity of phosphorothioate siRNAs

(2015) Hartmut Jahns et al.   Nature Communications

Multivalent N-Acetylgalactosamine-Conjugated siRNA Localizes in Hepatocytes and Elicits Robust RNAi-Mediated Gene Silencing

(2014) Jayaprakash K. Nair et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Synthesis, biophysical properties and biological activity of second generation antisense oligonucleotides containing chiral phosphorothioate linkages

(2014) W. Brad Wan et al.   NUCLEIC ACIDS RESEARCH

Targeted delivery of antisense oligonucleotides to hepatocytes using triantennaryN-acetyl galactosamine improves potency 10-fold in mice

(2014) Thazha P. Prakash et al.   NUCLEIC ACIDS RESEARCH

Phosphorothioates, Essential Components of Therapeutic Oligonucleotides

(2014) Fritz Eckstein   Nucleic Acid Therapeutics

Stereocontrolled synthesis of oligonucleotide analogs containing chiral internucleotidic phosphorus atoms

(2011) Natsuhisa Oka et al.   CHEMICAL SOCIETY REVIEWS

Click chemistry with DNA

(2010) Afaf H. El-Sagheer et al.   CHEMICAL SOCIETY REVIEWS

A large-scale chemical modification screen identifies design rules to generate siRNAs with high activity, high stability and low toxicity

(2009) Jesper B. Bramsen et al.   NUCLEIC ACIDS RESEARCH

Stereocontrolled Synthesis of Oligoribonucleoside Phosphorothioates by an Oxazaphospholidine Approach

(2009) Natsuhisa Oka et al.   ORGANIC LETTERS

Chemical Modification of siRNAs for In Vivo Use

(2008) Mark A. Behlke   OLIGONUCLEOTIDES