Details of the Target

General Information of Target

Target ID LDTP03192
Target Name Nuclear receptor subfamily 4immunitygroup A member 1 (NR4A1)
Gene Name NR4A1
Gene ID 3164
Synonyms
GFRP1; HMR; NAK1; Nuclear receptor subfamily 4immunitygroup A member 1; Early response protein NAK1; Nuclear hormone receptor NUR/77; Nur77; Orphan nuclear receptor HMR; Orphan nuclear receptor TR3; ST-59; Testicular receptor 3
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MPCIQAQYGTPAPSPGPRDHLASDPLTPEFIKPTMDLASPEAAPAAPTALPSFSTFMDGY
TGEFDTFLYQLPGTVQPCSSASSSASSTSSSSATSPASASFKFEDFQVYGCYPGPLSGPV
DEALSSSGSDYYGSPCSAPSPSTPSFQPPQLSPWDGSFGHFSPSQTYEGLRAWTEQLPKA
SGPPQPPAFFSFSPPTGPSPSLAQSPLKLFPSQATHQLGEGESYSMPTAFPGLAPTSPHL
EGSGILDTPVTSTKARSGAPGGSEGRCAVCGDNASCQHYGVRTCEGCKGFFKRTVQKNAK
YICLANKDCPVDKRRRNRCQFCRFQKCLAVGMVKEVVRTDSLKGRRGRLPSKPKQPPDAS
PANLLTSLVRAHLDSGPSTAKLDYSKFQELVLPHFGKEDAGDVQQFYDLLSGSLEVIRKW
AEKIPGFAELSPADQDLLLESAFLELFILRLAYRSKPGEGKLIFCSGLVLHRLQCARGFG
DWIDSILAFSRSLHSLLVDVPAFACLSALVLITDRHGLQEPRRVEELQNRIASCLKEHVA
AVAGEPQPASCLSRLLGKLPELRTLCTQGLQRIFYLKLEDLVPPPPIIDKIFMDTLPF
Target Type
Literature-reported
Target Bioclass
Transcription factor
Family
Nuclear hormone receptor family, NR4 subfamily
Subcellular location
Nucleus
Function
Orphan nuclear receptor. Binds the NGFI-B response element (NBRE) 5'-AAAGGTCA-3'. Binds 9-cis-retinoic acid outside of its ligand-binding (NR LBD) domain. Participates in energy homeostasis by sequestrating the kinase STK11 in the nucleus, thereby attenuating cytoplasmic AMPK activation. Regulates the inflammatory response in macrophages by regulating metabolic adaptations during inflammation, including repressing the transcription of genes involved in the citric acid cycle (TCA). Inhibits NF-kappa-B signaling by binding to low-affinity NF-kappa-B binding sites, such as at the IL2 promoter. May act concomitantly with NR4A2 in regulating the expression of delayed-early genes during liver regeneration. Plays a role in the vascular response to injury.; In the cytosol, upon its detection of both bacterial lipopolysaccharide (LPS) and NBRE-containing mitochondrial DNA released by GSDMD pores during pyroptosis, it promotes non-canonical NLRP3 inflammasome activation by stimulating association of NLRP3 and NEK7.
TTD ID
T41119
Uniprot ID
P22736
DrugMap ID
TTMXE2Q
Ensemble ID
ENST00000243050.5
HGNC ID
HGNC:7980
ChEMBL ID
CHEMBL1293229

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT15 SNV: p.R345W .
HEC1 Deletion: p.L26Ter .
Ishikawa (Heraklio) 02 ER SNV: p.T48A; p.C566R .
MCC13 SNV: p.S98F .
NCIH446 SNV: p.C78F .
RL952 SNV: p.S129F .
RPMI7951 SNV: p.P96R .
SNGM SNV: p.G271V .

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  		C316(1.49)  LDD3427  [1]
IA-alkyne
 Probe Info  		C551(18.86)  LDD1706  [2]
TFBX
 Probe Info  		C3(0.00); C566(0.00); C551(0.00)  LDD0027  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 T cell-activated C551(5.49)  LDD1708  [2]
 LDCM0023  KB03 G-361 C547(10.17)  LDD2746  [1]
 LDCM0024  KB05 SK-MEL-28 C316(1.49)  LDD3427  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein arginine N-methyltransferase 1 (PRMT1) Protein arginine N-methyltransferase family Q99873
Glycerol kinase (GK) FGGY kinase family P32189
Ankyrin repeat and IBR domain-containing protein 1 (ANKIB1) RBR family Q9P2G1
LON peptidase N-terminal domain and RING finger protein 1 (LONRF1) . Q17RB8
Transporter and channel
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Apoptosis regulator Bcl-2 (BCL2) Bcl-2 family P10415
Exportin-1 (XPO1) Exportin family O14980
ADP/ATP translocase 1 (SLC25A4) Mitochondrial carrier (TC 2.A.29) family P12235
BCL2/adenovirus E1B 19 kDa protein-interacting protein 3-like (BNIP3L) NIP3 family O60238
Cellular tumor antigen p53 (TP53) P53 family P04637
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Signal transducer and activator of transcription 3 (STAT3) Transcription factor STAT family P40763
Transcription factor p65 (RELA) . Q04206
Other
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclin-dependent kinase 4 inhibitor D (CDKN2D) CDKN2 cyclin-dependent kinase inhibitor family P55273
Protein CutA (CUTA) CutA family O60888
Vasodilator-stimulated phosphoprotein (VASP) Ena/VASP family P50552
Keratin-associated protein 10-5 (KRTAP10-5) KRTAP type 10 family P60370
Plexin-D1 (PLXND1) Plexin family Q9Y4D7
Tubulin beta-4A chain (TUBB4A) Tubulin family P04350
Matrin-3 (MATR3) . P43243
PiggyBac transposable element-derived protein 1 (PGBD1) . Q96JS3

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 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255