Structural highlights
Function
VDRA_DANRE Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Regulates transcription of hormone sensitive genes via its association with the WINAC complex, a chromatin-remodeling complex. Plays a central role in calcium homeostasis.[1]
Publication Abstract from PubMed
We synthesized UG-650, a novel non-Gemini analog of UVB1 that combines structural features of UVB1 and MC 1288. The evaluation of the bioactivities indicates that UG-650 dose-dependently inhibited MCF-7 cell proliferation. In comparison to calcitriol, slightly lower concentrations of UG-650 were needed to achieve equivalent levels of proliferation inhibition. Structural analysis revealed that the analog forms additional interactions stabilizing VDR active form.
Design, synthesis and biological evaluation of a novel non-Gemini analog of UVB1 and crystal structure of its complex with the vitamin D receptor.,Gomez-Bouzo U, Peluso-Iltis C, Santalla H, Verlinden L, Verstuyf A, Rochel N, Gomez G, Fall Y Bioorg Chem. 2025 Apr;157:108239. doi: 10.1016/j.bioorg.2025.108239. Epub 2025 , Feb 4. PMID:39938446[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Ciesielski F, Rochel N, Moras D. Adaptability of the Vitamin D nuclear receptor to the synthetic ligand Gemini: remodelling the LBP with one side chain rotation. J Steroid Biochem Mol Biol. 2007 Mar;103(3-5):235-42. Epub 2007 Jan 10. PMID:17218092 doi:http://dx.doi.org/10.1016/j.jsbmb.2006.12.003
- ↑ Gómez-Bouzó U, Peluso-Iltis C, Santalla H, Verlinden L, Verstuyf A, Rochel N, Gómez G, Fall Y. Design, synthesis and biological evaluation of a novel non-Gemini analog of UVB1 and crystal structure of its complex with the vitamin D receptor. Bioorg Chem. 2025 Apr;157:108239. PMID:39938446 doi:10.1016/j.bioorg.2025.108239
