ArticleBiomacromolecules2010
Rational design of targeted cancer therapeutics through the multiconjugation of folate and cleavable siRNA to RAFT-synthesized (HPMA-s-APMA) copolymers.
Article in Biomacromolecules, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Covalent Polymer-RNA Conjugates for Potent Activation of the RIG-I Pathway.Advanced healthcare materials · 2025Article
- Beyond Lipids: Exploring Advances in Polymeric Gene Delivery in the Lipid Nanoparticles Era.Advanced materials (Deerfield Beach, Fla.) · 2024Review
- Systemically Administered TLR7/8 Agonist and Antigen-Conjugated Nanogels Govern Immune Responses against Tumors.ACS nano · 2022Article
- Enhanced control of bioactivity of tissue plasminogen activator (tPA) through domain-directed enzymatic oxidation of terminal galactose.BioImpacts : BI · 2022Article
- Thiolated-Polymer-Based Nanoparticles as an Avant-Garde Approach for Anticancer Therapies-Reviewing Thiomers from Chitosan and Hyaluronic Acid.Pharmaceutics · 2021Review
- Cellular uptake and targeting of low dispersity, dual emissive, segmented block copolymer nanofibers.Chemical science · 2020Article
- Determinants of preferential renal accumulation of synthetic polymers in acute kidney injury.International journal of pharmaceutics · 2019Article
- Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo Delivery.Molecules (Basel, Switzerland) · 2019Review
- RGD-decorated cholesterol stabilized polyplexes for targeted siRNA delivery to glioblastoma cells.Drug delivery and translational research · 2019Article
- Synthesis of 5'-Thio-3'-O-ribonucleoside Phosphoramidites.The Journal of organic chemistry · 2017Article
- Reduction Sensitive PEG Hydrogels for Codelivery of Antigen and Adjuvant To Induce Potent CTLs.Molecular pharmaceutics · 2016Article
- Folate receptor-targeted aminoglycoside-derived polymers for transgene expression in cancer cells.Bioengineering & translational medicine · 2016Article
- Decationized polyplexes as stable and safe carrier systems for improved biodistribution in systemic gene therapy.Journal of controlled release : official journal of the Controlled Release Society · 2014Article
- Glucose-containing diblock polycations exhibit molecular weight, charge, and cell-type dependence for pDNA delivery.Biomacromolecules · 2014Article
- Application of living free radical polymerization for nucleic acid delivery.Accounts of chemical research · 2012Article
- Reductively responsive siRNA-conjugated hydrogel nanoparticles for gene silencing.Journal of the American Chemical Society · 2012Article
- Non-condensing polymeric nanoparticles for targeted gene and siRNA delivery.International journal of pharmaceutics · 2012Review
- Guanidine-Containing Methacrylamide (Co)polymers via aRAFT: Toward a Cell Penetrating Peptide Mimic().ACS macro letters · 2012Article
- Hybrid hydrogels self-assembled from graft copolymers containing complementary β-sheets as hydroxyapatite nucleation scaffolds.Biomaterials · 2011Article
- Synthesis of folate-functionalized RAFT polymers for targeted siRNA delivery.Biomacromolecules · 2011Article
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3 authors.
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Abstract
A well-defined N-(2-hydroxypropyl)methacrylamide-s-N-(3-aminopropyl)methacrylamide (HPMA-s-APMA) copolymer, synthesized via reversible addition-fragmentation chain transfer (RAFT) polymerization, was utilized for the rational design of multiconjugates containing both a gene therapeutic, small interfering RNA (siRNA), and a cancer cell targeting moiety, folate. The copolymer contains a biocompatible poly(HPMA) portion (91 mol %) and a primary amine, APMA, portion (9 mol %). A fraction (20 mol %) of the APMA repeats were converted to activated thiols utilizing the amine- and sulfhydryl-reactive molecule N-succinimidyl 3-(2-pyridyldithio)-propionate (SPDP). 5'-Thiolated sense strand RNAs were then coupled to the polymer through a disulfide exchange with pendant pyridyldithio moieties, giving an 89 +/- 4% degree of conjugation. The unmodified APMA units (80 mol %) were subsequently coupled to amine reactive folates with 81 +/- 1% efficiency. This yielded a multiconjugate copolymer with 91 mol % HPMA, 2 mol % RNA, and 6 mol % folate. siRNA formation was achieved by annealing antisense strands to the conjugated RNA sense strands. Subsequent siRNA cleavage under intracellular conditions demonstrated the potential utility of this carrier in gene delivery. The multiconjugate copolymer and siRNA release were characterized by UV-vis spectroscopy and polyacrylamide gel electrophoresis.
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