General Information of Target

Target ID LDTP02670
Target Name Retinoic acid receptor gamma (RARG)
Gene Name RARG
Gene ID 5916
Synonyms
NR1B3; Retinoic acid receptor gamma; RAR-gamma; Nuclear receptor subfamily 1 group B member 3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MATNKERLFAAGALGPGSGYPGAGFPFAFPGALRGSPPFEMLSPSFRGLGQPDLPKEMAS
LSVETQSTSSEEMVPSSPSPPPPPRVYKPCFVCNDKSSGYHYGVSSCEGCKGFFRRSIQK
NMVYTCHRDKNCIINKVTRNRCQYCRLQKCFEVGMSKEAVRNDRNKKKKEVKEEGSPDSY
ELSPQLEELITKVSKAHQETFPSLCQLGKYTTNSSADHRVQLDLGLWDKFSELATKCIIK
IVEFAKRLPGFTGLSIADQITLLKAACLDILMLRICTRYTPEQDTMTFSDGLTLNRTQMH
NAGFGPLTDLVFAFAGQLLPLEMDDTETGLLSAICLICGDRMDLEEPEKVDKLQEPLLEA
LRLYARRRRPSQPYMFPRMLMKITDLRGISTKGAERAITLKMEIPGPMPPLIREMLENPE
MFEDDSSQPGPHPNASSEDEVPGGQGKGGLKSPA
Target Type
Successful
Target Bioclass
Transcription factor
Family
Nuclear hormone receptor family, NR1 subfamily
Subcellular location
Nucleus
Function
Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence of ligand, acts mainly as an activator of gene expression due to weak binding to corepressors. Required for limb bud development. In concert with RARA or RARB, required for skeletal growth, matrix homeostasis and growth plate function.
TTD ID
T82146
Uniprot ID
P13631
DrugMap ID
TT1Q3IE
Ensemble ID
ENST00000338561.9
HGNC ID
HGNC:9866
ChEMBL ID
CHEMBL2003

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HKGZCC SNV: p.D385N DBIA    Probe Info 
JURKAT SNV: p.R115H .

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 
C54(1.38)  LDD3312  [1]
NAIA_5
 Probe Info 
C205(0.00); C203(0.00)  LDD2224  [2]
IPM
 Probe Info 
N.A.  LDD2156  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 8305C C54(1.70)  LDD2248  [1]
 LDCM0023  KB03 8305C C54(2.21)  LDD2665  [1]
 LDCM0024  KB05 HMCB C54(1.38)  LDD3312  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Bardet-Biedl syndrome 4 protein (BBS4) BBS4 family Q96RK4
Transcription factor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Retinoic acid receptor RXR-beta (RXRB) Nuclear hormone receptor family P28702
Retinoic acid receptor RXR-gamma (RXRG) Nuclear hormone receptor family P48443
Myogenic factor 5 (MYF5) . P13349
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
cAMP-dependent protein kinase type I-beta regulatory subunit (PRKAR1B) CAMP-dependent kinase regulatory chain family P31321

The Drug(s) Related To This Target

Approved
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acitretin Small molecular drug DB00459
Adapalene Small molecular drug DB00210
Alitretinoin Small molecular drug D0G3PI
Isotretinoin Small molecular drug DB00982
Tazarotene Small molecular drug D0BM5G
Tretinoin Small molecular drug D02DGU
Trifarotene Small molecular drug D06FOU
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Palovarotene Small molecular drug D0H8OH
Investigative
Click To Hide/Show 14 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
3-fluoro-4-{[(2r)-2-hydroxy-2-(5588-tetramethyl-5678-tetrahydro-2-naphthalenyl)Acetyl]Amino}Benzoic Acid Small molecular drug DB07031
Agn193109 Small molecular drug D0Q0IR
Ahpn Small molecular drug D0A6NQ
Bms184394 Small molecular drug D0OM2S
Bms270394 Small molecular drug D0M3LK
Cd2665 Small molecular drug D0Y6WJ
Cd564 Small molecular drug D0O6QU
Cd666 Small molecular drug D0F8CC
Dodecyl-alpha-d-maltoside Small molecular drug D05DWG
Mm 11253 Small molecular drug D06RAM
Sr11254 Small molecular drug D0E3SB
3-fluoro-4-[2-hydroxy-2-(5588-tetramethyl-5678-tetrahydro-naphtalen-2-yl)-acetylamino]-benzoic Acid . DB07294
Bms-181156 . DB02466
Lgd-1550 . DB05785
Patented
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid27336223-compound-11 Small molecular drug D0W8JK
Pmid27336223-compound-12 Small molecular drug D09YFJ
Pmid27336223-compound-13 Small molecular drug D01OYE
Pmid27336223-compound-14 Small molecular drug D0MC3J
Pmid27336223-compound-15 Small molecular drug D0YP0T
Pmid27336223-compound-9 Small molecular drug D0ZQ0X
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Etretinate Small molecular drug DB00926

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 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
3 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019