ArticleBritish journal of cancer1998
The antiproliferative activity of all-trans-retinoic acid catabolites and isomers is differentially modulated by liarozole-fumarate in MCF-7 human breast cancer cells.
Article in British journal of cancer, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 31 citations in OpenAlex.
- Elevated expression of endocan in the development of cervical squamous neoplasia of the uterus.Medical molecular morphology · 2023Article
- Retinoic acid metabolism in cancer: potential feasibility of retinoic acid metabolism blocking therapy.Medical molecular morphology · 2023Review
- Vitamin A Inhibits Development of Dextran Sulfate Sodium-Induced Colitis and Colon Cancer in a Mouse Model.BioMed research international · 2016Article
- Association study between novel CYP26 polymorphisms and the risk of betel quid-related malignant oral disorders.TheScientificWorldJournal · 2015Article
- Liarozole inhibits transforming growth factor-β3--mediated extracellular matrix formation in human three-dimensional leiomyoma cultures.Fertility and sterility · 2014Article
- Therapeutic potential of the inhibition of the retinoic acid hydroxylases CYP26A1 and CYP26B1 by xenobiotics.Current topics in medicinal chemistry · 2013Review
- A sensitive and specific method for measurement of multiple retinoids in human serum with UHPLC-MS/MS.Journal of lipid research · 2012Article
- Cytochrome P450s in the regulation of cellular retinoic acid metabolism.Annual review of nutrition · 2011Review
- Endometriosis expresses a molecular pattern consistent with decreased retinoid uptake, metabolism and action.Human reproduction (Oxford, England) · 2011Article
- Oncogenic and cell survival properties of the retinoic acid metabolizing enzyme, CYP26A1.Oncogene · 2010Article
- Targeting cytochrome P450 enzymes: a new approach in anti-cancer drug development.Bioorganic & medicinal chemistry · 2007Review
- Inhibition of all-TRANS-retinoic acid metabolism by R116010 induces antitumour activity.British journal of cancer · 2002Article
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Authors and funding
7 authors at 3 institutions in 3 countries.
Funding
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Abstract
The clinical use of all-trans-retinoic acid (ATRA) in the treatment of cancer is significantly hampered by the prompt emergence of resistance, believed to be caused by increased ATRA catabolism. Inhibitors of ATRA catabolism may therefore prove valuable for cancer therapy. Liarozole-fumarate is an anti-tumour drug that inhibits the cytochrome P450-dependent catabolism of ATRA. ATRA, but also its naturally occurring catabolites, 4-oxo-ATRA and 5,6-epoxy-ATRA, as well as its stereoisomers, 9-cis-RA and 13-cis-RA, show significant antiproliferative activity in MCF-7 human breast cancer cells. To further elucidate its mechanism of action, we investigated whether liarozole-fumarate was able to enhance the antiproliferative activity of ATRA catabolites and isomers. Liarozole-fumarate alone up to a concentration of 10(-6) M had no effect on MCF-7 cell proliferation. However, in combination with ATRA or the ATRA catabolites, liarozole-fumarate (10(-6) M) significantly enhanced their antiproliferative activity. On the contrary, liarozole-fumarate (10(-6) M) was not able to potentiate the antiproliferative activity of the ATRA stereoisomers, most probably because of the absence of cytochrome P450-dependent catabolism. Together, these findings show that liarozole-fumarate acts as a versatile inhibitor of retinoid catabolism in that it not only blocks the breakdown of ATRA, but also inhibits the catabolic pathway of 4-oxo-ATRA and 5,6-epoxy-ATRA, thereby enhancing their antiproliferative activity.
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