Structural highlights
Function
VDR_RAT 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. Recruited to promoters via its interaction with the WINAC complex subunit BAZ1B/WSTF, which mediates the interaction with acetylated histones, an essential step for VDR-promoter association. Plays a central role in calcium homeostasis.[1]
Publication Abstract from PubMed
Vitamin D receptor (VDR) is a member of the nuclear receptor superfamily and regulates the expression of target genes through ligand binding. To express the target gene, coactivator binding to the VDR/ligand complex is essential. Although there are many coactivators in living cells, precise interactions between coactivators and VDR have not been clarified. Here, we synthesized two coactivator peptides, DRIP205-2 and SRC2-3, evaluated their affinity for the ligand-binding domain (LBD) of VDR using 1alpha,25-dihydroxyvitamin D3, partial agonist 1, and antagonist 2 by surface plasmon resonance (SPR), and assessed their interaction modes with VDR-LBD using X-ray crystallographic analysis. This study showed that the SRC2-3 peptide is more sensitive to the ligands (agonist, partial agonist, and antagonist) and shows more intimate interactions with VDR-LBD than DRIP205-2 peptide.
SRC2-3 binds to vitamin D receptor with high sensitivity and strong affinity.,Egawa D, Itoh T, Kato A, Kataoka S, Anami Y, Yamamoto K Bioorg Med Chem. 2017 Jan 15;25(2):568-574. doi: 10.1016/j.bmc.2016.11.020. Epub , 2016 Nov 14. PMID:27890450[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Vanhooke JL, Tadi BP, Benning MM, Plum LA, DeLuca HF. New analogs of 2-methylene-19-nor-(20S)-1,25-dihydroxyvitamin D3 with conformationally restricted side chains: evaluation of biological activity and structural determination of VDR-bound conformations. Arch Biochem Biophys. 2007 Apr 15;460(2):161-5. Epub 2006 Dec 12. PMID:17227670 doi:10.1016/j.abb.2006.11.029
- ↑ Egawa D, Itoh T, Kato A, Kataoka S, Anami Y, Yamamoto K. SRC2-3 binds to vitamin D receptor with high sensitivity and strong affinity. Bioorg Med Chem. 2017 Jan 15;25(2):568-574. doi: 10.1016/j.bmc.2016.11.020. Epub , 2016 Nov 14. PMID:27890450 doi:http://dx.doi.org/10.1016/j.bmc.2016.11.020
