ArticleChemistry (Weinheim an der Bergstrasse, Germany)2017
A pH-sensitive Macromolecular Prodrug as TLR7/8 Targeting Immune Response Modifier.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
What it found
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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
14 citing papers in PubMed, 26 citations in OpenAlex.
- TLR8 Stimulation Leads to Microenvironment Activation and Enhanced Antibody-Dependent Cellular Responses in CLL.International journal of molecular sciences · 2026Article
- Review
- Precise delivery and controlled release: strategies and advances in TLR7/8 agonist prodrugs for cancer immunotherapy.Frontiers in immunology · 2026Review
- Dissecting the Efficacy and Immunogenicity of TLR7 Agonist-Antibody Conjugates through the Lens of Fc Effector Function, Conjugation Strategies, and Linker Cleavability.Journal of medicinal chemistry · 2025Article
- Polyphosphazene-Based Nanotherapeutics.Journal of functional biomaterials · 2025Review
- Design and Evaluation of Synthetic Delivery Formulations for Peptide-Based Cancer Vaccines.BME frontiers · 2024Article
- Biomimetic virus-like mesoporous silica nanoparticles improved cellular internalization for co-delivery of antigen and agonist to enhance Tumor immunotherapy.Drug delivery · 2023Article
- Design and Characterization of Immune-Stimulating Imidazo[4,5-c]quinoline Antibody-Drug Conjugates.Molecular pharmaceutics · 2022Article
- Systemic Immunotherapy with Micellar Resiquimod-Polymer Conjugates Triggers a Robust Antitumor Response in a Breast Cancer Model.Advanced healthcare materials · 2021Article
- Polyphosphazene immunoadjuvants: Historical perspective and recent advances.Journal of controlled release : official journal of the Controlled Release Society · 2021Review
- Supramolecular assembly of Toll-like receptor 7/8 agonist into multimeric water-soluble constructs enables superior immune stimulationACS applied bio materials · 2020Article
- Main-Chain Phosphorus-Containing Polymers for Therapeutic Applications.Molecules (Basel, Switzerland) · 2020Review
- Stimuli-Responsive Phosphorus-Based Polymers.European journal of inorganic chemistry · 2019Review
- A pH-sensitive Macromolecular Prodrug as TLR7/8 Targeting Immune Response Modifier.Chemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 3 countries.
Funding
Abstract
The chemical synthesis and biological activity of novel functionalized imidazoquinoline derivatives (ImQ) to generate Toll-like receptor (TLR) 7/8 specific prodrugs are presented. In vivo activity of ImQs to induce inflammation was confirmed in zebrafish larvae. After covalent ligation to fully biodegradable polyphosphazenes (ImQ-polymer), the macromolecular prodrugs were designed to undergo intracellular pH-sensitive release of ImQs to induce inflammation through binding to endosomal TLR7/8 (danger signal). We showed ImQ dissociation from prodrugs at a pH 5 pointing towards endosomal prodrug degradability. ImQ-polymers strongly activated ovalbumin-specific T cells in murine splenocytes as shown by increased proliferation and expression of the IL-2 receptor (CD25) on CD8+ T cells accompanied by strong IFN-γ release. ImQ prodrugs presented here are suggested to form the basis of novel nanovaccines, for example, for intravenous or intratumoral cancer immunotherapeutic applications to trigger physiological antitumor immune responses.
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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.