ArticleThe Biochemical journal2009
A putrescine-anthracene conjugate: a paradigm for selective drug delivery.
Article in The Biochemical journal, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 32 citations in OpenAlex.
- Novel Water-Soluble, Heavy Atom-Free Thioxanthene-Fused Naphthalimide-Polyamine Phototheranostic Conjugates.ChemMedChem · 2026Article
- Biogenic Polyamines and Related Metabolites.Biomolecules · 2021Article
- The salivary metatranscriptome as an accurate diagnostic indicator of oral cancer.NPJ genomic medicine · 2021Article
- Solid-Phase Synthesis of Selectively Mono-Fluorobenz(o)ylated Polyamines as a Basis for the Development ofMolecules (Basel, Switzerland) · 2021Article
- Identification ofFrontiers in medicine · 2019Article
- Polyamines - A New Metabolic Switch: Crosstalk With Networks Involving Senescence, Crop Improvement, and Mammalian Cancer Therapy.Frontiers in plant science · 2019Article
- Anthracene-polyamine conjugates inhibit in vitro proliferation of intraerythrocytic Plasmodium falciparum parasites.Antimicrobial agents and chemotherapy · 2013Article
- Polyamine pathway inhibition as a novel therapeutic approach to treating neuroblastoma.Frontiers in oncology · 2012Article
- Polyamine homoeostasis as a drug target in pathogenic protozoa: peculiarities and possibilities.The Biochemical journal · 2011Review
- Current status of the polyamine research field.Methods in molecular biology (Clifton, N.J.) · 2011Review
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 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Increased polyamine concentrations play an important role in the development of cancer at all stages, from initiation through to maintenance of the transformed phenotype. One way cancer cells accumulate increased concentrations of polyamines is by increased uptake of preformed polyamines via their PTS (polyamine transport system). The PTS is promiscuous and will transport a range of polyamine-based molecules. Therefore it may be that cytotoxic drugs could be attached to polyamine vectors and targeted selectively to cancer cells by utilizing the PTS. The aim of the present study was to investigate the potential of Ant 4, a putrescine-anthracene conjugate, to target cytotoxic agents to human cancer cells as a paradigm for a novel method of selective drug delivery. Ant 4 induced cytotoxicity after only 24 h exposure. Apoptosis was the predominant type of cell death, with mechanistic studies revealing that oxidative stress and DNA damage may have a part to play. For the first time, uptake of Ant 4 via the PTS was demonstrated both directly and indirectly in human cell lines. In addition, Ant 4 significantly reduced putrescine uptake, demonstrating that this conjugate not only used the PTS, but also could successfully compete with its native polyamine for uptake. However, the most interesting finding was the intracellular depletion of the polyamine pools, providing an additional mode of toxicity for Ant 4 and the possibility that this molecule may act as a 'double-edged sword': preventing cell growth by delivery of the toxic moiety and by depletion of intracellular polyamine content.
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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.