Details of the Target

General Information of Target

Target ID LDTP02572
Target Name Vitamin D3 receptor (VDR)
Gene Name VDR
Gene ID 7421
Synonyms
NR1I1; Vitamin D3 receptor; VDR; 1,25-dihydroxyvitamin D3 receptor; Nuclear receptor subfamily 1 group I member 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEAMAASTSLPDPGDFDRNVPRICGVCGDRATGFHFNAMTCEGCKGFFRRSMKRKALFTC
PFNGDCRITKDNRRHCQACRLKRCVDIGMMKEFILTDEEVQRKREMILKRKEEEALKDSL
RPKLSEEQQRIIAILLDAHHKTYDPTYSDFCQFRPPVRVNDGGGSHPSRPNSRHTPSFSG
DSSSSCSDHCITSSDMMDSSSFSNLDLSEEDSDDPSVTLELSQLSMLPHLADLVSYSIQK
VIGFAKMIPGFRDLTSEDQIVLLKSSAIEVIMLRSNESFTMDDMSWTCGNQDYKYRVSDV
TKAGHSLELIEPLIKFQVGLKKLNLHEEEHVLLMAICIVSPDRPGVQDAALIEAIQDRLS
NTLQTYIRCRHPPPGSHLLYAKMIQKLADLRSLNEEHSKQYRCLSFQPECSMKLTPLVLE
VFGNEIS
Target Type
Successful
Target Bioclass
Transporter and channel
Family
Nuclear hormone receptor family, NR1 subfamily
Subcellular location
Nucleus
Function
Nuclear receptor for calcitriol, the active form of vitamin D3 which mediates the action of this vitamin on cells. Enters the nucleus upon vitamin D3 binding where it forms heterodimers with the retinoid X receptor/RXR. The VDR-RXR heterodimers bind to specific response elements on DNA and activate the transcription of vitamin D3-responsive target genes. Plays a central role in calcium homeostasis. Also functions as a receptor for the secondary bile acid lithocholic acid (LCA) and its metabolites.
TTD ID
T34234
Uniprot ID
P11473
DrugMap ID
TTK59TV
Ensemble ID
ENST00000395324.6
HGNC ID
HGNC:12679
ChEMBL ID
CHEMBL1977

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AN3CA SNV: p.R402H .
CCK81 SNV: p.A6V .
IGR1 SNV: p.E329K .
IM95 SNV: p.S298G .
KNS42 SNV: p.M196I .
LS180 SNV: p.P122H .
MFE319 SNV: p.H330R .
MOLT4 SNV: p.R274C .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C84(1.22)  LDD3373  [1]
IA-alkyne
 Probe Info  		C403, C410(20.00); C151(14.42)  LDD1704  [2]
NAIA_5
 Probe Info  		N.A.  LDD2223  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 T cell-activated C403, C410(20.00); C151(14.42)  LDD1704  [2]
 LDCM0023  KB03 A-375 C84(2.07)  LDD2672  [1]
 LDCM0024  KB05 OCUG-1 C84(1.22)  LDD3373  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Pachytene checkpoint protein 2 homolog (TRIP13) AAA ATPase family Q15645
Protein N-terminal glutamine amidohydrolase (NTAQ1) NTAQ1 family Q96HA8
Ribosomal protein S6 kinase delta-1 (RPS6KC1) Ser/Thr protein kinase family Q96S38
Tyrosine-protein phosphatase non-receptor type 3 (PTPN3) Protein-tyrosine phosphatase family P26045
Nuclear receptor coactivator 1 (NCOA1) SRC/p160 nuclear receptor coactivator family Q15788
Histone acetyltransferase p300 (EP300) . Q09472
OTU domain-containing protein 4 (OTUD4) . Q01804
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cellular tumor antigen p53 (TP53) P53 family P04637
Transcription factor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Retinoic acid receptor RXR-alpha (RXRA) Nuclear hormone receptor family P19793
Retinoic acid receptor RXR-gamma (RXRG) Nuclear hormone receptor family P48443
Homeobox protein MOX-2 (MEOX2) . P50222
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Mediator of RNA polymerase II transcription subunit 1 (MED1) Mediator complex subunit 1 family Q15648
SNW domain-containing protein 1 (SNW1) SNW family Q13573
Sequestosome-1 (SQSTM1) . Q13501

The Drug(s) Related To This Target

Approved
Click To Hide/Show 14 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alfacalcidol Small molecular drug DB01436
Calcidiol Small molecular drug D02VPX
Calcifediol Small molecular drug DB00146
Calcipotriol Small molecular drug D01QUS
Calcitriol Small molecular drug D0T2PL
Cholecalciferol Small molecular drug D0K5WS
Cholesterol Small molecular drug DB04540
Curcumin Small molecular drug DB11672
Dihydrotachysterol Small molecular drug D0G8OC
Doxercalciferol Small molecular drug D0G5CF
Ergocalciferol Small molecular drug D06JPB
Falecalcitrol Small molecular drug D01UFN
Paricalcitol Small molecular drug D0N1TP
Vitamin D . DB11094
Phase 3
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Seocalcitol Small molecular drug D09ZJQ
S-06911 . D0U8CR
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Inecalcitol Oral Small molecular drug D0R8IE
Phase 1
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ro-23-7553 Small molecular drug D00CGH
Ctap-201 . D05SOH
Investigative
Click To Hide/Show 18 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
2md Small molecular drug D02EHY
3-keto-lithocholic Acid Small molecular drug D06RBG
Calcitriol-26,23-lactone Small molecular drug D06DEL
Elocalcitol Small molecular drug DB06194
Gemini Small molecular drug D0K8VA
Inecalcitol Small molecular drug DB04796
Ksp-bcs-1-alpha-chf2-1624f2-2 Small molecular drug D0X3DK
Ksp-bcs-1-alpha-chf2-20-epi-22-oxabishomo-26-oh Small molecular drug D0XZ2P
Lg190178 Small molecular drug D07AHG
Mc-1301 Small molecular drug D0C7NV
Tei-9647 Small molecular drug D0D6XV
Zk159222 Small molecular drug D0X0AM
(1r3r)-5-[(2e)-3-{(1s3r)-223-trimethyl-3-[666-trifluoro-5-hydroxy-5-(Trifluoromethyl)Hex-3-yn-1-yl]Cyclopentyl}Prop-2-en-1-ylidene]Cyclohexane-13-diol . DB07530
13-cyclohexanediol 4-methylene-5-[(2e)-[(1s3as7as)-octahydro-1-(5-hydroxy-5-methyl-13-hexadiynyl)-7a-methyl-4h-inden-4-ylidene]Ethylidene]- (1r3s5z) . DB08742
Becocalcidiol . DB04891
Cta018 . DB05024
Curcumin Sulfate . DB14635
Eldecalcitol . DB05295
Patented
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid27454349-compound-100 Small molecular drug D0P1KV
Pmid27454349-compound-101 Small molecular drug D0WT4I
Pmid27454349-compound-102 Small molecular drug D0O2HK
Pmid27454349-compound-91 Small molecular drug D0UK7K
Pmid27454349-compound-92 Small molecular drug D0P8CM
Pmid27454349-compound-93 Small molecular drug D09KWM
Pmid27454349-compound-94 Small molecular drug D0WV1W
Pmid27454349-compound-95 Small molecular drug D0JC8M
Pmid27454349-compound-96 Small molecular drug D0UY3J
Pmid27454349-compound-97 Small molecular drug D03ZXP
Pmid27454349-compound-98 Small molecular drug D00SZR
Pmid27454349-compound-99 Small molecular drug D0PJ2C
Discontinued
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Atocalcitol Small molecular drug D06SBK
Ecalcidene Small molecular drug D0O6WJ
Lexacalcitol Small molecular drug D0RF9T
Ro-26-9228 Small molecular drug D0I4GI
Tisocalcitate Small molecular drug D07BDY
Bxl-746 . D08KZR
Cb-1267 . D0KK4U
Cep-4186 . D0T9SJ

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
3 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264