The calcitriol receptor, also known as the vitamin D receptor (VDR) and also known as NR1I1 (nuclear receptor subfamily 1, group I, member 1), is a member of the nuclear receptor family of transcription factors. Upon activation by vitamin D, the VDR forms a heterodimer with the retinoid-X receptor and binds to hormone response elements on DNA resulting in expression or transrepression of specific geneproducts. The VDR not only regulates transcriptional responses but also involved in microRNA-directed post transcriptional mechanisms.

An overview of VD/VDR

Vitamin D receptor (VDR), belonging to the superfamily, is a nucleophilic protein and is an endogenous biomolecule that mediates 1, 25(OH), D and exerts biological effects. Studies have shown that the VDR gene from the amino terminal to the carboxyl terminal can be generally divided into six functional regions, A, B, C, D, E and F, and each of them has a different division of labor but also cooperates with others. Many biological functions of vitamin D are achieved through VDR-mediated regulation of target gene transcription. 1, 25(OH), D hormone signaling molecules bind to VDR to form a hormone-receptor complex, which acts on specific DNA sequences on target genes and regulates the expression of structural genes. And VDR is an essential ligand-dependent nuclear transcription factor, which plays an important role in maintaining calcium-phosphorus metabolism and regulating cell proliferation and differentiation.

Major types of VD/VDR

VDR can be divided into nuclear receptor (nVDR) and cell membrane receptor (mVDR), whose molecular weight is 50KDa and 60KDa respectively.

Activation of VD/VDR

As the active form of vitamin D hormone, calcitriol is a non-selective activator of the vitamin D receptor. Its binding affinity to the vitamin D receptor (IC 50=0.4 nM) is more than 10 times that of the selective VDRA, paricalcitol.

VD/VDR and diseases

There is a close relationship between vitamin D and the etiology of asthma. Vitamin D can affect embryonic lung development, and can lead to imbalance of immune system with environmental risk factors. In addition, the 12th Q arm of VDR is similar to asthma-related regions, and its polymorphism is a very good marker for asthma. And genomic scanning found that VDR is a candidate gene associated with asthma. Besides, Th1/Th2 imbalance is one of the pathogenesis of asthma, and the level of IgE in mice with VDR receptor deficiency increased and TH2 level lowered. Vitamin D can inhibit the function of TH1 lymphocytes and enhance TH2 lymphocytes. In genetic association studies on populations, the variation of VDR gene may be closely related to the occurrence and development of asthma, and the polymorphism of different sites may be affected by race.

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