Vitamin D and New Vitamin D Analogs
A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".
Deadline for manuscript submissions: 30 November 2025 | Viewed by 38
Special Issue Editor
Interests: vitamin D; medicinal chemistry; organic chemistry synthesis; ionic liquids synthesis; bioactive compounds
Special Issue Information
Dear Colleagues,
The active form of Vitamin D3, 1α, 25-dihydroxyvitamin D3 (1,25 D or calcitriol), exerts its biological functions by binding to the vitamin D receptor (VDR), a transcription factor of the nuclear receptor (NR) superfamily. Calcitriol was known for many years as a primary regulator of calcium homeostasis, but it also controls a wide range of other biological functions, including cell differentiation, cell proliferation, and immune responses. It induces the expression of more than 200 genes associated with several diseases such as arthritis, diabetes, and cancer, suggesting that this hormone might induce a wide range of biological functions. Unfortunately, 1,25D induces hypercalcemia at the doses required for the treatment of hyperproliferative diseases such as cancer. This limitation has led to intense synthetic efforts towards VDR ligands with selective activities as potential therapeutic agents for the treatment of cancer, immunodeficiency syndromes, autoimmune diseases, and skin disorders. Calcipotriol and maxacalcitol, examples of 1,25D analogs with a modified side-chain, exhibit a similar or higher antiproliferative potency with reduced calcemic effects in comparison with natural hormone 1,25D. Other potent 1,25D analogs structurally modified at the CD-rings or triene system that induce low potency for calcium metabolism have also been synthesized. 1,25D therapeutic doses promote calcium absorption, leading to hypercalcemia. More than 4000 vitamin D analogs have been synthesized to dissociate the hypercalcemic effect from the anti-inflammatory and/or antiproliferative activities, but only a few of them have reached clinical application. There is accordingly still much interest in the design and synthesis of new calcitriol analogs exhibiting high cell-differentiating properties coupled with low or negligible calcemic effects.
Prof. Dr. Yagamare Fall
Guest Editor
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Keywords
- vitamin D
- vitamin D receptor
- vitamin D analogs
- synthesis
- clinical applications
- cancer
- anti-proliferation
- therapeutic target
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