8ck5
From Proteopedia
VDR LBD complex with 25-nitro derivative of 1,25D3
Structural highlights
FunctionVDRA_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 PubMedIntense synthetic efforts have been directed towards the development of noncalcemic analogs of 1,25-dihydroxyvitamin D(3). We describe here the structural analysis and biological evaluation of two derivatives of 1,25-dihydroxyvitamin D(3) with modifications limited to the replacement of the 25-hydroxyl group by a 25-amino or 25-nitro groups. Both compounds are agonists of the vitamin D receptor. They mediate biological effects similar to 1,25-dihydroxyvitamin D(3), the 25-amino derivative being the most potent one while being less calcemic than 1,25-dihydroxyvitamin D(3). The in vivo properties of the compounds make them of potential therapeutic value. Structural analysis and biological activities of C25-amino and C25-nitro vitamin D analogs.,Gomez-Bouzo U, Belorusova AY, Rivadulla ML, Santalla H, Verlinden L, Verstuyf A, Ferronato MJ, Curino AC, Facchinetti MM, Fall Y, Gomez G, Rochel N Bioorg Chem. 2023 Apr 6;136:106528. doi: 10.1016/j.bioorg.2023.106528. PMID:37054528[2] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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