ArticleMolecular pharmaceutics2012
Prodrug strategy for PSMA-targeted delivery of TGX-221 to prostate cancer cells.
Article in Molecular pharmaceutics, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 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
25 citing papers in PubMed, 57 citations in OpenAlex.
- Aptamers in Osteosarcoma: New Paths for Diagnosis and Treatment.Anti-cancer agents in medicinal chemistry · 2026Review
- Monoamine neurotransmitter functionalized poly(amidoamine) dendrimers for targeting of cabazitaxel to human prostate cancer cells.Discover nano · 2025Article
- SP1 Mediated PIK3CB Upregulation Promotes Gastric Carcinogenesis.Journal of Cancer · 2024Article
- Recent Advances in Dual PI3K/mTOR Inhibitors for Tumour Treatment.Frontiers in pharmacology · 2022Review
- Intra-Articular injection of acid-sensitive stearoxyl-ketal-dexamethasone microcrystals for long-acting arthritis therapy.Asian journal of pharmaceutical sciences · 2021Article
- Improved Anti-Triple Negative Breast Cancer Effects of Docetaxel by RGD-Modified Lipid-Core Micelles.International journal of nanomedicine · 2021Article
- Review
- Characterization of a novel p110β-specific inhibitor BL140 that overcomes MDV3100-resistance in castration-resistant prostate cancer cells.The Prostate · 2017Article
- In Vitro and In Vivo Efficacy Studies of Lavender angustifolia Essential Oil and Its Active Constituents on the Proliferation of Human Prostate Cancer.Integrative cancer therapies · 2017Article
- Lipid-Drug Conjugate for Enhancing Drug Delivery.Molecular pharmaceutics · 2017Review
- Targeted delivery of ginsenoside compound K using TPGS/PEG-PCL mixed micelles for effective treatment of lung cancer.International journal of nanomedicine · 2017Article
- The therapeutic and diagnostic potential of the prostate specific membrane antigen/glutamate carboxypeptidase II (PSMA/GCPII) in cancer and neurological disease.British journal of pharmacology · 2016Review
- Enhancing DPYSL3 gene expression via a promoter-targeted small activating RNA approach suppresses cancer cell motility and metastasis.Oncotarget · 2016Article
- Utilization of Enzyme-Immobilized Mesoporous Silica Nanocontainers (IBN-4) in Prodrug-Activated Cancer Theranostics.Nanomaterials (Basel, Switzerland) · 2015Article
- Nanoparticle-mediated delivery of a rapidly activatable prodrug of SN-38 for neuroblastoma therapy.Biomaterials · 2015Article
- Nanomicellar TGX221 blocks xenograft tumor growth of prostate cancer in nude mice.The Prostate · 2015Article
- Prostate cancer relevant antigens and enzymes for targeted drug delivery.Journal of controlled release : official journal of the Controlled Release Society · 2014Review
- Cell-type-specific, Aptamer-functionalized Agents for Targeted Disease Therapy.Molecular therapy. Nucleic acids · 2014Article
- PI3K-AKT-mTOR-signaling and beyond: the complex network in gastroenteropancreatic neuroendocrine neoplasms.Theranostics · 2014Review
- Aptamer-conjugated nanomaterials for specific cancer cell recognition and targeted cancer therapy.NPG Asia materials · 2014Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit. Recent studies showed that TGX-221 has antiproliferative activity against PTEN-deficient tumor cell lines including prostate cancers. The objective of this study was to develop an encapsulation system for parenterally delivering TGX-221 to the target tissue through a prostate-specific membrane aptamer (PSMAa10) with little or no side effects. In this study, PEG-PCL micelles were formulated to encapsulate the drug, and a prodrug strategy was pursued to improve the stability of the carrier system. Fluorescence imaging studies demonstrated that the cellular uptake of both drug and nanoparticles was significantly improved by targeted micelles in a PSMA positive cell line. The area under the plasma concentration time curve of the micelle formulation in nude mice was 2.27-fold greater than that of the naked drug, and the drug clearance rate was 6.16-fold slower. These findings suggest a novel formulation approach for improving site-specific drug delivery of a molecular-targeted prostate cancer treatment.
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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.