ArticleInternational journal of molecular sciences2016
Antiproliferative Activity of Double Point Modified Analogs of 1,25-Dihydroxyvitamin D₂ Against Human Malignant Melanoma Cell Lines.
Article in International journal of molecular sciences, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 26 citations in OpenAlex.
- Influence of genetic variants of the vitamin D receptor on clinical profile in cirrhosis and hepatocellular carcinoma.Ecancermedicalscience · 2025Article
- Anticancer Activity of Vitamin D, Lumisterol and Selected Derivatives against Human Malignant Melanoma Cell Lines.International journal of molecular sciences · 2024Article
- Review
- The Chemoprotective Role of Vitamin D in Skin Cancer: A Systematic Review.Cancer management and research · 2022Review
- Vitamin D Enhances Anticancer Properties of Cediranib, a VEGFR Inhibitor, by Modulation of VEGFR2 Expression in Melanoma Cells.Frontiers in oncology · 2021Article
- Current Molecular Markers of Melanoma and Treatment Targets.International journal of molecular sciences · 2020Review
- Serum Total 25-Hydroxyvitamin D Levels in Patients With Cutaneous Malignant Melanoma: A Case-Control Study in a Low-Risk Southern European Population.Dermatology practical & conceptual · 2020Article
- Relevance of Vitamin D in Melanoma Development, Progression and Therapy.Anticancer research · 2020Review
- Vitamin D and Its Synthetic Analogs.Journal of medicinal chemistry · 2019Review
- Vitamin D and its low calcemic analogs modulate the anticancer properties of cisplatin and dacarbazine in the human melanoma A375 cell line.International journal of oncology · 2019Article
- Antiproliferative Activity of Non-Calcemic Vitamin D Analogs on Human Melanoma Lines in Relation to VDR and PDIA3 Receptors.International journal of molecular sciences · 2018Article
- Vitamins D: Relationship between Structure and Biological Activity.International journal of molecular sciences · 2018Review
- Vitamin D and Its Analogues Decrease Amyloid-β (Aβ) Formation and Increase Aβ-Degradation.International journal of molecular sciences · 2017Article
- Associations between abnormal vitamin D metabolism pathway function and non-small cell lung cancer.Oncology letters · 2017Article
- Melanoma Chemoprevention: Current Status and Future Prospects.Photochemistry and photobiology · 2017Review
- 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
- Longitudinal, observational study on associations between postoperative nutritional vitamin D supplementation and clinical outcomes in esophageal cancer patients undergoing esophagectomy.Scientific reports · 2016Observational
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Vitamin D is a lipid soluble steroid hormone with pleiotropic biological properties, including regulation of cell proliferation, differentiation and apoptosis. As to these desirable anticancer actions, 1,25-dihydroxyvitamins D and analogs have been reported to inhibit the proliferation and to induce differentiation of a wide variety of cancer cell types, including human malignant melanoma. However, there is a need for novel and more efficacious vitamin D analogs, and how best to design such is still an open issue. A series of double point modified (DPM) analogs of 1,25-dihydroxyvitamin D₂ (1,25(OH)₂D₂) induced differentiation of the vitamin D receptor (VDR) positive A375 and VDR negative SK-MEL 188b human malignant melanoma cell lines. Surprisingly, the dose of 1,25(OH)₂D₂ required to inhibit the proliferation of the A375 melanoma cell line by was several fold lower than that required in the case of 1,25(OH)₂D₃. To evaluate the impact of the modification in the side chain (additional 22-hydroxyl) and in the A-ring (5,6-trans modification), the regular side-chain of vitamin D₂ or D₃ was retained in the structure of our analogs. As expected, 5,6-trans modification was advantageous to enhancing the anti-proliferative activity of analogs, but not as a single point modification (SPM). Very unexpectedly, the additional 22-hydroxyl in the side-chain reduced significantly the anti-proliferative activity of both the natural and 5,6-trans series analogs. Finally, an induction of pigmentation in melanoma SK-MEL 188b cells was observed to sensitized cells to the effect of vitamin D analogs.
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Registered trials
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