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8ckc

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Vitamin D receptor complex with 25-amine derivative of 1,25D3

Structural highlights

8ckc is a 2 chain structure with sequence from Danio rerio and Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	,
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

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

Intense 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

↑ 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, Belorusova AY, Rivadulla ML, Santalla H, Verlinden L, Verstuyf A, Ferronato MJ, Curino AC, Facchinetti MM, Fall Y, Gómez G, Rochel N. Structural analysis and biological activities of C25-amino and C25-nitro vitamin D analogs. Bioorg Chem. 2023 Apr 6;136:106528. PMID:37054528 doi:10.1016/j.bioorg.2023.106528