ArticleChemical science2017
Controlled in-cell activation of RNA therapeutics using bond-cleaving bio-orthogonal chemistry.
Article in Chemical science, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
20 citing papers in PubMed, 44 citations in OpenAlex.
- Programmable nanomedicine via bioorthogonal molecular engineering.Nano convergence · 2026Review
- Spatiotemporally controlled drug release via a click-release system utilizing mono-alkyl-hydroxylamine and cyclooctyne chemistry.Nature communications · 2026Article
- Precise Regulations at the Subcellular Level through Intracellular Polymerization, Assembly, and Transformation.JACS Au · 2024Review
- Trans-cyclooctene-a Swiss army knife for bioorthogonal chemistry: exploring the synthesis, reactivity, and applications in biomedical breakthroughs.EJNMMI radiopharmacy and chemistry · 2024Review
- Direct Activation of Nucleobases with Small Molecules for the Conditional Control of Antisense Function.Angewandte Chemie (International ed. in English) · 2024Article
- Senolysis Enabled by Senescent Cell-Sensitive Bioorthogonal Tetrazine Ligation.Angewandte Chemie (International ed. in English) · 2024Article
- Bioorthogonal PROTAC Prodrugs Enabled by On-Target Activation.Journal of the American Chemical Society · 2023Article
- Building bioorthogonal click-release capable artificial receptors on cancer cell surface for imaging, drug targeting and delivery.Acta pharmaceutica Sinica. B · 2023Article
- Tetrazine-Induced Bioorthogonal Activation of Vitamin E-Modified siRNA for Gene Silencing.Molecules (Basel, Switzerland) · 2022Article
- Chemical synthesis of stimuli-responsive guide RNA for conditional control of CRISPR-Cas9 gene editing.Chemical science · 2021Article
- Structurally Redesigned Bioorthogonal Reagents for Mitochondria-Specific Prodrug Activation.JACS Au · 2021Article
- Click activated protodrugs against cancer increase the therapeutic potential of chemotherapy through local capture and activation.Chemical science · 2021Article
- Activation and Delivery of Tetrazine-Responsive Bioorthogonal Prodrugs.Molecules (Basel, Switzerland) · 2020Review
- Synthetic methodology towards allylicChemical science · 2020Article
- Postsynthetic On-Column 2' Functionalization of RNA by Convenient Versatile Method.International journal of molecular sciences · 2020Article
- Switchable Fluorescence of Doxorubicin for Label-Free Imaging of Bioorthogonal Drug Release.ChemMedChem · 2020Article
- Aryl Azides as Phosphine-Activated Switches for Small Molecule Function.Scientific reports · 2019Article
- At the Intersection of Biomaterials and Gene Therapy: Progress in Non-viral Delivery of Nucleic Acids.Frontiers in bioengineering and biotechnology · 2019Review
- Chemically triggered drug release from an antibody-drug conjugate leads to potent antitumour activity in mice.Nature communications · 2018Article
- Stimuli-responsive oligonucleotides in prodrug-based approaches for gene silencing.Beilstein journal of organic chemistry · 2018Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Temporal control of siRNA activation is a major challenge for RNAi-based therapeutics. The majority of the reported siRNA delivery systems rely on environmental factors, such as differences in extracellular and intracellular redox potential, ATP concentration, or pH to activate an siRNA payload. However dynamic endogenous environments are far too complex to rely on for controllable siRNA release and can result in premature siRNA activation prior to reaching the intended biological target. In addition, there are uncertainties about timing, degree and rate of the siRNA activation with spontaneous release approaches. Herein we describe a bio-orthogonal chemistry approach to address this important challenge. With our approach we were able achieve two major goals: complete siRNA inactivation upon immobilization of the payload on the surface of iron oxide nanoparticles and controlled in-cell activation with the addition of a small non-toxic chemical trigger after sufficient cellular uptake of the nanoparticles was confirmed. We have demonstrated our in-cell activation approach using two siRNAs against green fluorescent protein (GFP) and cyclin dependent kinase 8 (CDK8) in GFP expressing MDA-MB-231 cell line. We anticipate that this methodology will potentially advance the clinical translation of RNAi-based therapeutics, as the described bio-orthogonal chemistry can be generalized for any siRNA of choice.
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.