ArticleBritish journal of cancer2002
Inhibition of all-TRANS-retinoic acid metabolism by R116010 induces antitumour activity.
Article in British journal of cancer, 2002. 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, 84 citations in OpenAlex.
- Frontiers in manganese catalysis: a sustainable platform for bond construction and heterocycle synthesis.RSC advances · 2026Review
- Recent Advances in the Application of 2-Aminobenzothiazole to the Multicomponent Synthesis of Heterocycles.ChemistryOpen · 2024Review
- Cu(ii)-catalyzed C-N coupling of 2-aminobenzothiazoles with boronic acids at room temperature.RSC advances · 2023Article
- Liposomal delivery of hydrophobic RAMBAs provides good bioavailability and significant enhancement of retinoic acid signalling in neuroblastoma tumour cells.Journal of drug targeting · 2020Article
- Efficiency of All-Trans Retinoic Acid on Gastric Cancer: A Narrative Literature Review.International journal of molecular sciences · 2018Review
- Imidazoles as potential anticancer agents.MedChemComm · 2017Review
- Transcription factor TLX1 controls retinoic acid signaling to ensure spleen development.The Journal of clinical investigation · 2016Article
- Improved Homology Model of the Human all-trans Retinoic Acid Metabolizing Enzyme CYP26A1.Molecules (Basel, Switzerland) · 2016Article
- Role of Retinoic Acid-Metabolizing Cytochrome P450s, CYP26, in Inflammation and Cancer.Advances in pharmacology (San Diego, Calif.) · 2015Review
- Therapeutic potential of the inhibition of the retinoic acid hydroxylases CYP26A1 and CYP26B1 by xenobiotics.Current topics in medicinal chemistry · 2013Review
- First chemical feature-based pharmacophore modeling of potent retinoidal retinoic acid metabolism blocking agents (RAMBAs): identification of novel RAMBA scaffolds.European journal of medicinal chemistry · 2012Article
- Cytochrome P450s in the regulation of cellular retinoic acid metabolism.Annual review of nutrition · 2011Review
- Substrate specificity and ligand interactions of CYP26A1, the human liver retinoic acid hydroxylase.Molecular pharmacology · 2011Article
- The role of CYP26 enzymes in retinoic acid clearance.Expert opinion on drug metabolism & toxicology · 2009Review
- A novel role for the retinoic acid-catabolizing enzyme CYP26A1 in Barrett's associated adenocarcinoma.Oncogene · 2008Article
- Molecular targeting of retinoic acid metabolism in neuroblastoma: the role of the CYP26 inhibitor R116010 in vitro and in vivo.British journal of cancer · 2007Article
- Novel retinoic acid metabolism blocking agents have potent inhibitory activities on human breast cancer cells and tumour growth.British journal of cancer · 2007Article
- Inhibitory effects of retinoic acid metabolism blocking agents (RAMBAs) on the growth of human prostate cancer cells and LNCaP prostate tumour xenografts in SCID mice.British journal of cancer · 2006Article
- Increasing the intracellular availability of all-trans retinoic acid in neuroblastoma cells.British journal of cancer · 2005Article
- Review
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Authors and funding
15 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
All-trans-retinoic acid is a potent inhibitor of cell proliferation and inducer of differentiation. However, the clinical use of all-trans-retinoic acid in the treatment of cancer is significantly hampered by its toxicity and the prompt emergence of resistance, believed to be caused by increased all-trans-retinoic acid metabolism. Inhibitors of all-trans-retinoic acid metabolism may therefore prove valuable in the treatment of cancer. In this study, we characterize R116010 as a new anticancer drug that is a potent inhibitor of all-trans-retinoic acid metabolism. In vitro, R116010 potently inhibits all-trans-retinoic acid metabolism in intact T47D cells with an IC(50)-value of 8.7 nM. In addition, R116010 is a selective inhibitor as indicated by its inhibition profile for several other cytochrome P450-mediated reactions. In T47D cell proliferation assays, R116010 by itself has no effect on cell proliferation. However, in combination with all-trans-retinoic acid, R116010 enhances the all-trans-retinoic acid-mediated antiproliferative activity in a concentration-dependent manner. In vivo, the growth of murine oestrogen-independent TA3-Ha mammary tumours is significantly inhibited by R116010 at doses as low as 0.16 mg kg(-1). In conclusion, R116010 is a highly potent and selective inhibitor of all-trans-retinoic acid metabolism, which is able to enhance the biological activity of all-trans-retinoic acid, thereby exhibiting antitumour activity. R116010 represents a novel and promising anticancer drug with an unique mechanism of action.
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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.