ArticleBiochemical pharmacology2012
Rat CYP24A1 acts on 20-hydroxyvitamin D(3) producing hydroxylated products with increased biological activity.
Article in Biochemical pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
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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.
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Who cites it
36 citing papers in PubMed, 44 citations in OpenAlex.
- 1,24,25(OH)Scientific reports · 2025Article
- Anticancer Activity of Vitamin D, Lumisterol and Selected Derivatives against Human Malignant Melanoma Cell Lines.International journal of molecular sciences · 2024Article
- Biological Effects of CYP11A1-Derived Vitamin D and Lumisterol Metabolites in the Skin.The Journal of investigative dermatology · 2024Review
- Review
- CYP11A1‑derived vitamin D hydroxyderivatives as candidates for therapy of basal and squamous cell carcinomas.International journal of oncology · 2022Article
- Chemical synthesis, biological activities and action on nuclear receptors of 20S(OH)DBioorganic chemistry · 2022Article
- Is Vitamin D Deficiency Related to Increased Cancer Risk in Patients with Type 2 Diabetes Mellitus?International journal of molecular sciences · 2021Review
- Vitamin D and lumisterol derivatives can act on liver X receptors (LXRs).Scientific reports · 2021Article
- Detection of 7-Dehydrocholesterol and Vitamin D3 Derivatives in Honey.Molecules (Basel, Switzerland) · 2020Article
- Relevance of Vitamin D in Melanoma Development, Progression and Therapy.Anticancer research · 2020Review
- The Role of Classical and Novel Forms of Vitamin D in the Pathogenesis and Progression of Nonmelanoma Skin Cancers.Advances in experimental medicine and biology · 2020Review
- The serum vitamin D metabolome: What we know and what is still to discover.The Journal of steroid biochemistry and molecular biology · 2019Review
- CYP27A1 acts on the pre-vitamin D3 photoproduct, lumisterol, producing biologically active hydroxy-metabolites.The Journal of steroid biochemistry and molecular biology · 2018Article
- Exploring vitamin D metabolism and function in cancer.Experimental & molecular medicine · 2018Review
- Properties of purified CYP2R1 in a reconstituted membrane environment and its 25-hydroxylation of 20-hydroxyvitamin D3.The Journal of steroid biochemistry and molecular biology · 2018Article
- On the role of classical and novel forms of vitamin D in melanoma progression and management.The Journal of steroid biochemistry and molecular biology · 2018Review
- Investigation of 20S-hydroxyvitamin DScientific reports · 2018Article
- Vitamin D signaling and melanoma: role of vitamin D and its receptors in melanoma progression and management.Laboratory investigation; a journal of technical methods and pathology · 2017Review
- Epigenetic and genetic dissections of UV-induced global gene dysregulation in skin cells through multi-omics analyses.Scientific reports · 2017Article
- Noncalcemic 20-hydroxyvitamin D3 inhibits human melanoma growth in in vitro and in vivo models.Oncotarget · 2017Article
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
Abstract
20-Hydroxyvitamin D(3) (20(OH)D(3)), the major product of CYP11A1 action on vitamin D(3), is biologically active and is produced in vivo. As well as potentially having important physiological actions, it is of interest as a therapeutic agent due to its lack of calcemic activity. In the current study we have examined the ability of CYP24A1, the enzyme that inactivates 1,25-dihydroxyvitamin D(3) (1,25(OH)(2)D(3)), to metabolize 20(OH)D(3). Rat CYP24A1 was expressed in Escherichia coli, purified by Ni-affinity chromatography and assayed with substrates incorporated into phospholipid vesicles which served as a model of the inner mitochondrial membrane. In this system CYP24A1 metabolized 1,25(OH)(2)D(3) with a catalytic efficiency 1.4-fold higher than that seen for 25-hydroxyvitamin D(3) (25(OH)D(3)). CYP24A1 hydroxylated 20(OH)D(3) to several dihydroxy-derivatives with the major two identified by NMR as 20,24-dihydroxyvitamin D(3) (20,24(OH)(2)D(3)) and 20,25-dihydroxyvitamin D(3) (20,25(OH)(2)D(3)). The catalytic efficiency of CYP24A1 for 20(OH)D(3) metabolism was more than 10-fold lower than for either 25(OH)D(3) or 1,25(OH)(2)D(3) and no secondary metabolites were produced. The two major products, 20,24(OH)(2)D(3) and 20,25(OH)(2)D(3), caused significantly greater inhibition of colony formation by SKMEL-188 melanoma cells than either 1,25(OH)(2)D(3) or the parent 20(OH)D(3), showing that CYP24A1 plays an activating, rather than an inactivating role on 20(OH)D(3).
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