Vitamin D Receptor (VDR) belongs to the nuclear receptor (NR) superfamily. Whereas the structure of the ligand binding domain (LBD) of VDR has been determined in great detail, the role of its amino acid residues in stabilizing the structure and ligand triggering conformational change is still under debate. There are 13 α-helices and one β-sheet in the VDR LBD and they form a three-layer sandwich structure stabilized by 10 residues. Thirty-six amino acid residues line the ligand binding pocket (LBP) and six of these residues have hydrogen-bonds linking with the ligand. In 1α,25-dihydroxyvitamin D 3 signaling, H3 and H12 play an important role in the course of conformational change resulting in the provision of interfaces for dimerization, coactivator (CoA), corepressor (CoR), and hTAF II 28. In this paper we provide a detailed description of the amino acid residues stabilizing the structure and taking part in conformational change of VDR LBD according to functional domains.

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An Fe-catalyzed unprotected hydroxylamine mediated Heck-type coupling between sulfinic acids and alkenes furnished structurally important (E)-vinyl sulfones with moderate to good yields, high atom-economy and regioselectivity.

Hepatic fibrosis is a reversible process involving plenty of transcription factors and pathways. Vitamin D receptor (VDR) as a member of ligand-induced transcription factors can interact with 9-cis retinoid X receptor (RXR) and VDR-interacting repressor (VDIR) to mediate transactivation or transrepression in the absence or in the presence of VDR ligand to regulate the expression of VDR target genes. The active form of vitamin D [1α,25(OH)2D3] can downregulate the expression of type I collagen both α1 and α2 (COLIα1 and COLIα2) in hepatic stellate cells (HSC-T6) in a time-dependent fashion, which provides a new direction for hepatic fibrosis therapy. As one of VDR target genes, rat COLIα1 gene contains 1αnVDRE (E-box1 and E-box2) in its promoter, and unliganded VDR/RXR may bind to 1αnVDRE through VDIR to mediate transactivation, whereas liganded VDR/RXR may bind to 1αnVDRE through VDIR for transrepression. The results suggested a sort of relying on each other relationship between VDR/RXR and VDIR in regulating the expression of COLIα1 gene in HSC-T6 cells, which established VDR as a potential target for blocking and even reversing hepatic fibrosis.

In this study, 9-anthracenemethyl methacrylate (AMMA) and styrene (St) as monomers and benzoyl peroxide as an initiator were used to synthesize P(St-co-AMMA), a macromolecule tracer with a fluorescence effect, via free radical copolymerization. A fluorescent online detection device was built on the basis of the principle of fluorescence online detection by using the single-screw extrusion platform of a torque rheometer to explore the effect of the amount of macromolecular tracer and screw speed on the residence time distribution of polystyrene in single-screw extrusion. Fourier transform infrared spectroscopy, 1H-NMR, thermal stability, fluorescence properties, and rheological properties show that the resulting product P(St-co-AMMA) has a degree of thermal stability, fluorescence, and rheological properties similar to polystyrene, so this product can be used to characterize the residence time distribution during single-screw extrusion. The amount of macromolecular tracer P(St-co-AMMA) does not affect the residence time distribution of polystyrene during single-screw extrusion processing, meanwhile, the minimum residence time decreases and the residence time distribution becomes narrow as the screw speed increases, that is, the axial mixing capacity of the single-screw extruder decreases as the screw speed increases.