ArticleInternational journal of nanomedicine2013
High-efficiency liposomal encapsulation of a tyrosine kinase inhibitor leads to improved in vivo toxicity and tumor response profile.
Article in International journal of nanomedicine, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 33 citations in OpenAlex.
- Staurosporine as an Antifungal Agent.International journal of molecular sciences · 2025Review
- Modulating hormonally upregulated neu-associated kinase (HUNK) activity in breast cancer: The development of HUNK inhibitors.The Journal of pharmacology and experimental therapeutics · 2025Review
- Epstein-Barr virus latent membrane protein 1 subverts IMPDH pathways to drive B-cell oncometabolism.PLoS pathogens · 2025Article
- The Inhibition Effect and Mechanism of Staurosporine Isolated fromMarine drugs · 2024Article
- Integration of FRET and sequencing to engineer kinase biosensors from mammalian cell libraries.Nature communications · 2021Article
- Chemo-immune synergetic therapy of esophageal carcinoma: trastuzumab modified, cisplatin and fluorouracil co-delivered lipid-polymer hybrid nanoparticles.Drug delivery · 2020Article
- Critical role of EphA3 in cancer and current state of EphA3 drug therapeutics.Molecular biology reports · 2020Review
- Article
- Development and Characterization of the Solvent-Assisted Active Loading Technology (SALT) for Liposomal Loading of Poorly Water-Soluble Compounds.Pharmaceutics · 2019Review
- Liposomal Taro Lectin Nanocapsules Control Human Glioblastoma and Mammary Adenocarcinoma Cell Proliferation.Molecules (Basel, Switzerland) · 2019Article
- Nanoformulations of anticancer FGFR inhibitors with improved therapeutic index.Nanomedicine : nanotechnology, biology, and medicine · 2018Article
- Staurosporine: new lease of life for parent compound of today's novel and highly successful anti-cancer drugs.The Journal of antibiotics · 2018Review
- Convergent Synthesis of N,S-bis Glycosylquinolin-2-ones via a Pd-G3-XantPhos Precatalyst Catalysis.Molecules (Basel, Switzerland) · 2018Article
- Microtubule affinity-regulating kinases are potential druggable targets for Alzheimer's disease.Cellular and molecular life sciences : CMLS · 2017Review
- Gold nanoparticles-based electrochemical method for the detection of protein kinase with a peptide-like inhibitor as the bioreceptor.International journal of nanomedicine · 2017Article
- A Simple and Improved Active Loading Method to Efficiently Encapsulate Staurosporine into Lipid-Based Nanoparticles for Enhanced Therapy of Multidrug Resistant Cancer.Pharmaceutical research · 2016Article
- Demonstration of Non-Gaussian Restricted Diffusion in Tumor Cells Using Diffusion Time-Dependent Diffusion-Weighted Magnetic Resonance Imaging Contrast.Frontiers in oncology · 2016Article
- Effect of the JAK2/STAT3 inhibitor SAR317461 on human glioblastoma tumorspheres.Journal of translational medicine · 2015Article
- Formulation design and evaluation of liposomal sepantronium bromide (YM155), a small-molecule survivin suppressant, based on pharmacokinetic modeling and simulation.Pharmaceutical research · 2015Article
- OX26/CTX-conjugated PEGylated liposome as a dual-targeting gene delivery system for brain glioma.Molecular cancer · 2014Article
Corrections and comments
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Authors and funding
13 authors at 2 institutions in 2 countries.
Funding
Abstract
Staurosporine (STS) is a potent pan-kinase inhibitor with marked activity against several chemotherapy-resistant tumor types in vitro. The translational progress of this compound has been hindered by poor pharmacokinetics and toxicity. We sought to determine whether liposomal encapsulation of STS would enhance antitumor efficacy and reduce toxicity, thereby supporting the feasibility of further preclinical development. We developed a novel reverse pH gradient liposomal loading method for STS, with an optimal buffer type and drug-to-lipid ratio. Our approach produced 70% loading efficiency with good retention, and we provide, for the first time, an assessment of the in vivo antitumor activity of STS. A low intravenous dose (0.8 mg/kg) inhibited U87 tumors in a murine flank model. Biodistribution showed preferential tumor accumulation, and body weight data, a sensitive index of STS toxicity, was unaffected by liposomal STS, but did decline with the free compound. In vitro experiments revealed that liposomal STS blocked Akt phosphorylation, induced poly(ADP-ribose) polymerase cleavage, and produced cell death via apoptosis. This study provides a basis to explore further the feasibility of liposomally encapsulated STS, and potentially related compounds for the management of resistant solid tumors.
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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.