Vitamin D3 receptor - Revision history

Wu3857: /* Reference */

2019-08-19T22:53:23Z

‎Reference

Wu3857: /* Cys Function & Property */

2019-08-19T20:50:22Z

‎Cys Function & Property

Wu3857 at 20:47, 19 August 2019

2019-08-19T20:47:42Z

Wu3857: /* Summary */

2019-08-19T20:47:09Z

‎Summary

Wu3857: Created page with "{| align="left" | TOC |} {{#invoke:InfoboxforTarget|run|VDR, NR1I1|[https://www.uniprot.org/uniprot/P11473 P11473]|Homo sapiens|Cys288|[http://pfam.xfam.org/family/PF0..."

2019-08-19T20:30:27Z

Created page with "{| align="left" | __TOC__ |} {{#invoke:InfoboxforTarget|run|VDR, NR1I1|[https://www.uniprot.org/uniprot/P11473 P11473]|Homo sapiens|Cys288|[http://pfam.xfam.org/family/PF0..."

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{| align="left"
| __TOC__
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{{#invoke:InfoboxforTarget|run|VDR, NR1I1|[https://www.uniprot.org/uniprot/P11473 P11473]|Homo sapiens|Cys288|[http://pfam.xfam.org/family/PF00104 Ligand-binding domain of nuclear hormone receptor], Nuclear hormone receptor family, NR1 subfamily|[[:Category:Vitamin D3 receptor|Ligand list]]|Transcription Related}}
==Summary==

===Protein Function ===
Vitamin D receptor (VDR), the nuclear receptor for 1α,25-dihydroxyvitamin D3 [1α,25-(OH)2D3], plays a pivotal role in the manifestation of multiple physiological properties of 1α,25-(OH)2D3, including calcium and phosphorus homeostasis, regulation of the immune response, and modulation of the growth and maturation of normal and malignant cells. 1α,25-(OH)2D3 binds VDR with high specificity and efficiency, allosterically promoting its heterodimerization with retinoid X receptor (RXR). The liganded dimer interacts with vitamin D response elements (VDREs) in the upstream promoter regions of vitamin D-regulated genes to trigger transcription and translation of the gene products. Since binding of 1α,25-(OH)2D3 to VDR must occur to initiate this cascade of physiological responses, analysis of the structure/function aspects of this interaction assumes major significance, especially in light of the fact that more than 500 analogues of 1α,25-(OH)2D3 have been synthesized and physiological effects of many were analyzed both in vitro and in vivo. (PMID: 11015194)</div>

===Cys Function & Property===
Cys288 is very close to the active site of VDR in space. 

* Hydrophobic property:
:[[File:574-hydro.png||600px]]
* SASA:
:Cys288: 18.529 A^2 

==Protein Sequence==

MEAMAASTSL PDPGDFDRNV PRICGVCGDR ATGFHFNAMT CEGCKGFFRR 
SMKRKALFTC PFNGDCRITK DNRRHCQACR LKRCVDIGMM KEFILTDEEV 
QRKREMILKR KEEEALKDSL RPKLSEEQQR IIAILLDAHH KTYDPTYSDF 
CQFRPPVRVN DGGGSHPSRP NSRHTPSFSG DSSSSCSDHC ITSSDMMDSS 
SFSNLDLSEE DSDDPSVTLE LSQLSMLPHL ADLVSYSIQK VIGFAKMIPG 
FRDLTSEDQI VLLKSSAIEV IMLRSNESFT MDDMSWT'''C'''GN QDYKYRVSDV 
TKAGHSLELI EPLIKFQVGL KKLNLHEEEH VLLMAICIVS PDRPGVQDAA 
LIEAIQDRLS NTLQTYIRCR HPPPGSHLLY AKMIQKLADL RSLNEEHSKQ 
YRCLSFQPEC SMKLTPLVLE VFGNEIS 


==Structural Information==
*Known structure with covalent ligand: 
:Unknown 

*Protein structure:
:[[File:574.png|center|800px]]

==Related Pathway==
*[https://www.genome.jp/kegg-bin/show_pathway?ko04928 Parathyroid hormone synthesis, secretion and action] 
*[https://www.genome.jp/kegg-bin/show_pathway?ko04961 Endocrine and other factor-regulated calcium reabsorption] 
*[https://www.genome.jp/kegg-bin/show_pathway?ko04978 Mineral absorption] 
*[https://www.genome.jp/kegg-bin/show_pathway?ko05152 Tuberculosis] 

==Experimental Evidence==
:Isotope Labeling, Homology Modeling, Molecular Docking

==Reference==
# Swamy N, Xu W, Paz N, et al. '''Molecular modeling, affinity labeling, and site-directed mutagenesis define the key points of interaction between the ligand-binding domain of the vitamin D nuclear receptor and 1α, 25-dihydroxyvitamin D3[J].''' Biochemistry, 2000, 39(40): 12162-12171. [https://www.ncbi.nlm.nih.gov/pubmed/?term=11015194 11015194] 

[[Category:Targets|Targets]]
[[Category:Homo sapiens|Homo sapiens]]
[[Category:Transcription Related|Transcription Related]]
[[Category:Nuclear hormone receptor family|Nuclear hormone receptor family]]
[[Category:NR1 subfamily|NR1 subfamily]]
[[Category:Parathyroid hormone synthesis, secretion and action|Parathyroid hormone synthesis, secretion and action]]
[[Category:Endocrine and other factor-regulated calcium reabsorption|Endocrine and other factor-regulated calcium reabsorption]]
[[Category:Mineral absorption|Mineral absorption]]
[[Category:Tuberculosis|Tuberculosis]]

@@ Line 48: / Line 48: @@
 # Swamy N, Xu W, Paz N, et al. '''Molecular modeling, affinity labeling, and site-directed mutagenesis define the key points of interaction between the ligand-binding domain of the vitamin D nuclear receptor and 1α, 25-dihydroxyvitamin D3[J].''' Biochemistry, 2000, 39(40): 12162-12171. [https://www.ncbi.nlm.nih.gov/pubmed/?term=11015194 11015194]<br/>
-[[Category:Targets|Targets]]
+[[Category:Targets]]
-[[Category:Homo sapiens|Homo sapiens]]
+[[Category:Homo sapiens]]
-[[Category:Transcription Related|Transcription Related]]
+[[Category:Transcription Related]]
-[[Category:Metabolic enzyme|Metabolic enzyme]]
+[[Category:Metabolic enzyme]]
-[[Category:Nuclear hormone receptor family|Nuclear hormone receptor family]]
+[[Category:Nuclear hormone receptor family]]
-[[Category:NR1 subfamily|NR1 subfamily]]
+[[Category:NR1 subfamily]]
-[[Category:Parathyroid hormone synthesis, secretion and action|Parathyroid hormone synthesis, secretion and action]]
+[[Category:Parathyroid hormone synthesis, secretion and action]]
-[[Category:Endocrine and other factor-regulated calcium reabsorption|Endocrine and other factor-regulated calcium reabsorption]]
+[[Category:Endocrine and other factor-regulated calcium reabsorption]]
-[[Category:Mineral absorption|Mineral absorption]]
+[[Category:Mineral absorption]]
-[[Category:Tuberculosis|Tuberculosis]]
+[[Category:Tuberculosis]]

@@ Line 14: / Line 14: @@
 :[[File:574-hydro.png||600px]]
 * SASA:
-:Cys288: 18.529 A^2<br/>
+:Cys288: 1.86 A^2<br/>
 ==Protein Sequence==

@@ Line 6: / Line 6: @@
 ===Protein Function ===
-Vitamin D receptor (VDR), the nuclear receptor for 1α,25-dihydroxyvitamin D3 [1α,25-(OH)<sub>2</sub>D<sub>3</sub>], plays a pivotal role in the manifestation of multiple physiological properties of 1α,25-(OH)<sub>2</sub>D<sub>3</sub>, including calcium and phosphorus homeostasis, regulation of the immune response, and modulation of the growth and maturation of normal and malignant cells. 1α,25-(OH)<sub>2</sub>D<sub>3</sub> binds VDR with high specificity and efficiency, allosterically promoting its heterodimerization with retinoid X receptor (RXR). The liganded dimer interacts with vitamin D response elements (VDREs) in the upstream promoter regions of vitamin D-regulated genes to trigger transcription and translation of the gene products. Since binding of 1α,25-(OH)<sub>2</sub>D<sub>3</sub> to VDR must occur to initiate this cascade of physiological responses, analysis of the structure/function aspects of this interaction assumes major significance, especially in light of the fact that more than 500 analogues of 1α,25-(OH)<sub>2</sub>D<sub>3</sub> have been synthesized and physiological effects of many were analyzed both in vitro and in vivo. (PMID: 11015194)</div>
+Vitamin D receptor (VDR), the nuclear receptor for 1α,25-dihydroxyvitamin D3 [1α,25-(OH)<sub>2</sub>D<sub>3</sub>], plays a pivotal role in the manifestation of multiple physiological properties of 1α,25-(OH)<sub>2</sub>D<sub>3</sub>, including calcium and phosphorus homeostasis, regulation of the immune response, and modulation of the growth and maturation of normal and malignant cells. 1α,25-(OH)<sub>2</sub>D<sub>3</sub> binds VDR with high specificity and efficiency, allosterically promoting its heterodimerization with retinoid X receptor (RXR). The liganded dimer interacts with vitamin D response elements (VDREs) in the upstream promoter regions of vitamin D-regulated genes to trigger transcription and translation of the gene products. Since binding of 1α,25-(OH)<sub>2</sub>D<sub>3</sub> to VDR must occur to initiate this cascade of physiological responses, analysis of the structure/function aspects of this interaction assumes major significance, especially in light of the fact that more than 500 analogues of 1α,25-(OH)<sub>2</sub>D<sub>3</sub> have been synthesized and physiological effects of many were analyzed both in vitro and in vivo. (PMID: 11015194)<br/>
 ===Cys Function & Property===