EB 1089, a Vitamin D Analogue, Induces the Vitamin D Receptor to Form Selective Receptor Complexes Depending on Cell Type

Vitamin D ◽  
1994 ◽  
pp. 255-256
Keyword(s):  
Vitamin D ◽  
Vitamin D Receptor ◽  
Cell Type ◽  
Receptor Complexes ◽  
Eb 1089 ◽  
Vitamin D Analogue

scholarly journals Cytosolic sequestration of the vitamin D receptor as a therapeutic option for vitamin D-induced hypercalcemia

2020 ◽  
Vol 11 (1) ◽  
Author(s):  
Daniela Rovito ◽  
Anna Y. Belorusova ◽  
Sandra Chalhoub ◽  
Anna-Isavella Rerra ◽  
Elvire Guiot ◽  
...  
Keyword(s):  
Vitamin D ◽  
Subcellular Localization ◽  
Vitamin D Receptor ◽  
Calcium Homeostasis ◽  
Calcium Intake ◽  
Target Genes ◽  
Therapeutic Option ◽  
Therapeutic Strategies ◽  
Circulating Levels ◽  
Vitamin D Analogue

AbstractThe bioactive vitamin D3, 1α,25(OH)2D3, plays a central role in calcium homeostasis by controlling the activity of the vitamin D receptor (VDR) in various tissues. Hypercalcemia secondary to high circulating levels of vitamin D3 leads to hypercalciuria, nephrocalcinosis and renal dysfunctions. Current therapeutic strategies aim at limiting calcium intake, absorption and resorption, or 1α,25(OH)2D3 synthesis, but are poorly efficient. In this study, we identify WBP4 as a new VDR interactant, and demonstrate that it controls VDR subcellular localization. Moreover, we show that the vitamin D analogue ZK168281 enhances the interaction between VDR and WBP4 in the cytosol, and normalizes the expression of VDR target genes and serum calcium levels in 1α,25(OH)2D3-intoxicated mice. As ZK168281 also blunts 1α,25(OH)2D3-induced VDR signaling in fibroblasts of a patient with impaired vitamin D degradation, this VDR antagonist represents a promising therapeutic option for 1α,25(OH)2D3-induced hypercalcemia.

Studies on the Interaction between the Vitamin D Receptor and the Radiolabelled 20-epi Vitamin D Analogue GS 1500

1998 ◽  
Vol 250 (2) ◽  
pp. 283-286 ◽  
Author(s):  
I.S. Mathiasen ◽  
G. Grue-Sørensen ◽  
C.Mørk Hansen ◽  
L. Binderup ◽  
F. Björkling
Keyword(s):  
Vitamin D ◽  
Vitamin D Receptor ◽  
Vitamin D Analogue

scholarly journals A phase I study of the vitamin D analogue EB 1089 in patients with advanced breast and colorectal cancer

1998 ◽  
Vol 78 (1) ◽  
pp. 6-13 ◽  
Author(s):  
T Gulliford ◽  
J English ◽  
KW Colston ◽  
P Menday ◽  
S Moller ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Vitamin D ◽  
Phase I ◽  
Phase I Study ◽  
Advanced Breast ◽  
Eb 1089 ◽  
Vitamin D Analogue

Vitamin D3 Derivatives with Adamantane or Lactone Ring Side Chains are Cell Type-Selective Vitamin D Receptor Modulators

2007 ◽  
Vol 71 (5) ◽  
pp. 1298-1311 ◽  
Author(s):  
Yuka Inaba ◽  
Keiko Yamamoto ◽  
Nobuko Yoshimoto ◽  
Manabu Matsunawa ◽  
Shigeyuki Uno ◽  
...  
Keyword(s):  
Vitamin D ◽  
Vitamin D Receptor ◽  
Vitamin D3 ◽  
Lactone Ring ◽  
Side Chains ◽  
Cell Type ◽  
Receptor Modulators

Isolation of Genomic DNA Sequences That Bind Vitamin D Receptor Complexes

2001 ◽  
Vol 283 (1) ◽  
pp. 188-194 ◽  
Author(s):  
Nicholas J. Koszewski ◽  
Stefan Kiessling ◽  
Hartmut H. Malluche
Keyword(s):  
Vitamin D ◽  
Vitamin D Receptor ◽  
Dna Sequences ◽  
Genomic Dna ◽  
Receptor Complexes
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