The hormonal form of vitamin D, 1α,25(OH)2-vitamin D3 (1α,25(OH)2D3), in addition of playing a central role in the control of calcium homeostasis in the body, regulates the growth and differentiation of different cell types, including cancer cells. At present several epidemiologic and clinical studies investigate the effect of the hormone in these cells due to the interest in the therapeutic use of 1α,25(OH)2D3 and analogues with less calcemic activity for prevention or treatment of cancer. This review describes vitamin D endocrine system, its mechanism of action, its antineoplastic activity and provides information about the latest advances in the study of new hormone analogues with less calcemic activity for cancer treatment.
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Synthetic Studies on Vitamin D Derivatives with Diverse but Selective Biological Activities.
Chem Pharm Bull (Tokyo)
January 2025
Faculty of Pharmaceutical Sciences, Teikyo University, 2-11-1 Kaga, Itabashi-ku, Tokyo 173-8605, Japan.
Article Synopsis
- A-ring modifications in 1α,25-dihydroxyvitamin D enhance its binding to the vitamin D receptor (VDR) and increase its stability in cells by resisting metabolism, leading to longer-lasting effects.
- Various modified A-ring precursors synthesized from d-glucose showed specific biological activities with minimal calcemic side effects, including MART-10's potent antitumor effects in cancer models and AH-1's superior bone-forming properties in osteoporosis models compared to natural vitamin D.
- Ongoing research includes developing a library of fluorinated vitamin D analogs with potential anti-inflammatory effects and therapeutic applications for conditions like psoriasis, alongside the creation of the VDR-silent analog KK-052, which selectively inhibits SREBP/SC
[Synthetic Studies on Bioactive Substances: From Research on Water-soluble Compounds to the Field of Lipophilic Ligands].
Yakugaku Zasshi
December 2024
Faculty of Pharmaceutical Sciences, Teikyo University.
This is a personal review of my chemistry research on retirement from Teikyo University. Under the guidance of Prof. Masaji Ohno of the Faculty of Pharmaceutical Sciences, The University of Tokyo, my research career started with the synthesis of water-soluble basic natural compounds, including the first artificial bleomycin showing potent molecular-oxygen activation effects and DNA binding abilities.
View Article and Find Full Text PDFThe vitamin D analog EB1089 sensitizes triple-negative breast cancer cells to the antiproliferative effects of antiestrogens.
Adv Med Sci
September 2024
Departamento de Biología Molecular y Biotecnología, Instituto de Investigaciones Biomédicas, Universidad Nacional Autónoma de México, Ciudad de México, 04510, Mexico; Programa de Investigación de Cáncer de Mama, Instituto de Investigaciones Biomédicas, Universidad Nacional Autónoma de México, Ciudad de México, 04510, Mexico. Electronic address:
Purpose: Patients bearing estrogen receptor (ER)α-negative breast cancer tumors confront poor prognosis and are typically unresponsive to hormone therapy. Previous studies have shown that calcitriol, the active vitamin D metabolite, can induce ERα expression in ERα-negative cells. EB1089, a calcitriol analog with reduced calcemic effects, exhibits greater potency than calcitriol in inhibiting cancer cell growth.
View Article and Find Full Text PDFStructure and the Anticancer Activity of Vitamin D Receptor Agonists.
Int J Mol Sci
June 2024
Department of Drug Chemistry Pharmaceutical and Biomedical Analysis, Faculty of Pharmacy, Medical University of Warsaw, 1 Stefana Banacha, 02-097 Warsaw, Poland.
Vitamin D is a group of seco-steroidal fat-soluble compounds. The two basic forms, vitamin D (ergocalciferol) and vitamin D (cholecalciferol), do not have biological activity. They are converted in the body by a two-step enzymatic hydroxylation into biologically active forms, 1α,25-dihydroxyvitamin D [ercalcitriol, 1,25(OH)D] and 1α,25-dihydroxyvitamin D [calcitriol, 1,25(OH)D], which act as classical steroid hormones.
View Article and Find Full Text PDFDesign, synthesis, and biological activity of D-bishomo-1α,25-dihydroxyvitamin D analogs and their crystal structures with the vitamin D nuclear receptor.
Eur J Med Chem
May 2024
Department of Biochemistry, University of Wisconsin-Madison, 433 Babcock Drive, Madison, WI, 53706, USA.
The biologically active metabolite of vitamin D - calcitriol - is a hormone involved in the regulation of calcium-phosphate homeostasis, immunological processes and cell differentiation, being therefore essential for the proper functioning of the human body. This suggests many applications of this steroid in the treatment of diseases such as rickets, psoriasis and some cancers. Unfortunately, using therapeutic doses of calcitriol is associated with high concentrations of this compound which causes hypercalcemia.
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