Related Experiment Video
Updated: Mar 26, 2026
Isolation of Mesenchymal Stem Cells from Human Alveolar Periosteum and Effects of Vitamin D on Osteogenic Activity of Periosteum-derived Cells
Published on: May 4, 2018
Vitamin D Analogs with Nitrogen Atom at C2 Substitution and Effect on Bone Formation
Atsushi Kittaka1, Masashi Takano1, Hiroshi Saitoh2
1Faculty of Pharmaceutical Sciences, Teikyo University, Tokyo, Japan.
Abstract:
The Arg274 residue of the ligand binding domain of human vitamin D receptor (hVDR) is important for 1α,25-dihydroxyvitamin D3 (1α,25(OH)2D3) binding as a specific ligand through forming a hydrogen bond with the 1α-OH group of the active vitamin D3, 1α,25(OH)2D3. An additional pincer-type hydrogen bond formation with Arg274 from a 2α-substituent of a synthetic 1α,25(OH)2D3 analog would enhance the binding affinity and biological activity. A series of 2α-[2-(heteroaryl)ethyl]-, 2α-(4-cyanobutyl)-, 2α-(ω-cyanoalkoxy)-, and 2β-(3-cyanopropoxy)-1α,25(OH)2D3 were designed and synthesized based on our original hVDR super agonists of 2α-(3-hydroxypropyl)- and 2α-(3-hydroxypropoxy)-1α,25(OH)2D3. Their potential biological activities, i.e., hVDR binding affinity, transactivation activity in HOS cells, and therapeutic effect on enhancing the bone mineral density of OVX rats, were studied.
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