Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNA Interference
Mutations

VDR (P11473) - Overview - Molecular Target Synopsis



Protein


VDR, Vitamin D3 receptor
UniProt P11473

Also Known as VDR_HUMAN, VDR, NR1I1

Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Recruited to promoters via its interaction with BAZ1B/WSTF which mediates the interaction with acetylated histones, an essential step for VDR-promoter association. Plays a central role in calcium homeostasis. Homodimer in the absence of bound vitamin D3. Heterodimer with RXRA after vitamin D3 binding. Interacts with SMAD3. Interacts with MED1, NCOA1, NCOA2, NCOA3 and NCOA6 coactivators, leading to a strong increase of transcription of target genes. Interacts (in a ligand-dependent manner) with BAZ1B/WSTF. Interacts with SNW1. Interacts with IRX4, the interaction doesn't affect its transactivation activity.

3X36 deposition date (2015-01-16)
CRYSTAL STRUCTURE OF THE HUMAN VITAMIN D RECEPTOR LIGAND BINDING DOMAIN COMPLEXED WITH 7,8-CIS-1A,25-DIHYDROXY-19-NORVITAMIN D3
RCSB/PDB
Inspect Structure
See all 3D Structures for VDR

Isoforms / Transcripts (Protein Coding)


Drugs


VDR is targeted by Approved Drugs Calcitriol, Cholecalciferol, Calcifediol, Calcipotriene, Ergocalciferol, Paricalcitol, Doxercalciferol. (see details)

Sub-cellular localization


UniProt: VDR is active in the following subcellular-locations: Nucleus.
GO terms: VDR is active in the following subcellular-locations: nucleoplasm, nucleus, receptor complex, RNA polymerase II transcription factor complex.



UniProt
GO terms

Mutations in Cancer


Please click the link to see mutations reported in COSMIC - Cell Lines Project
Please click the link to see mutations reported in COSMIC
Please click the link to see mutations reported in Cancer Gene Census
Please click the link to see mutations reported in ICGC
(see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H226, T47D, OVCAR_4

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: LS 180, LS 174T, SW 1463

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: HMEC, NHEK, NHLF

(see details)

RNA Interference


VDR was reported in the following RNAI studies:

AACR Journals - Results of primary druggable genome v2 (DG2) Achilles heel siRNA screen in KMS11 multiple myeloma cells, the highest RNAi cell lines are: KMS11. (see details)

Science - Cancer proliferation gene discovery through functional genomics, the highest RNAi cell lines are: HMECS. (see details)

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: . (see details)

3D Structures


There are 46 structures (49 chains) solved for VDR
42 are solved in complex with at least one small molecule ligand
3 are solved with an approved drug

VDR is solved in complex with the approved drug(s) VDX/Calcitriol (1DB1_A,1IE9_A,1RK3_A,2HC4_A,2ZLC_A,3M7R_A,3VT3_A,3VT7_A,4RUJ_A).
(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


VDR has been screened with 808 compounds (1590 bioactivities), 218 compounds have bioactivities that show binding affinity of <= 500nM (314 bioactivities). (see details)