Details of the Target

General Information of Target

Target ID LDTP02573
Target Name Steroid hormone receptor ERR1 (ESRRA)
Gene Name ESRRA
Gene ID 2101
Synonyms
ERR1; ESRL1; NR3B1; Steroid hormone receptor ERR1; Estrogen receptor-like 1; Estrogen-related receptor alpha; ERR-alpha; Nuclear receptor subfamily 3 group B member 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSSQVVGIEPLYIKAEPASPDSPKGSSETETEPPVALAPGPAPTRCLPGHKEEEDGEGAG
PGEQGGGKLVLSSLPKRLCLVCGDVASGYHYGVASCEACKAFFKRTIQGSIEYSCPASNE
CEITKRRRKACQACRFTKCLRVGMLKEGVRLDRVRGGRQKYKRRPEVDPLPFPGPFPAGP
LAVAGGPRKTAAPVNALVSHLLVVEPEKLYAMPDPAGPDGHLPAVATLCDLFDREIVVTI
SWAKSIPGFSSLSLSDQMSVLQSVWMEVLVLGVAQRSLPLQDELAFAEDLVLDEEGARAA
GLGELGAALLQLVRRLQALRLEREEYVLLKALALANSDSVHIEDAEAVEQLREALHEALL
EYEAGRAGPGGGAERRRAGRLLLTLPLLRQTAGKVLAHFYGVKLEGKVPMHKLFLEMLEA
MMD
Target Type
Successful
Target Bioclass
Transcription factor
Family
Nuclear hormone receptor family, NR3 subfamily
Subcellular location
Nucleus
Function
Binds to an ERR-alpha response element (ERRE) containing a single consensus half-site, 5'-TNAAGGTCA-3'. Can bind to the medium-chain acyl coenzyme A dehydrogenase (MCAD) response element NRRE-1 and may act as an important regulator of MCAD promoter. Binds to the C1 region of the lactoferrin gene promoter. Requires dimerization and the coactivator, PGC-1A, for full activity. The ERRalpha/PGC1alpha complex is a regulator of energy metabolism. Induces the expression of PERM1 in the skeletal muscle.
TTD ID
T72841
Uniprot ID
P11474
DrugMap ID
TTPNQAC
Ensemble ID
ENST00000000442.11
HGNC ID
HGNC:3471
ChEMBL ID
CHEMBL3429

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IPM
 Probe Info  		N.A.  LDD0241  [1]
NAIA_5
 Probe Info  		C46(0.74)  LDD2227  [2]
AHL-Pu-1
 Probe Info  		C46(3.93)  LDD0169  [3]
DBIA
 Probe Info  		C229(0.94); C46(1.04)  LDD1492  [4]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [5]
NAIA_4
 Probe Info  		N.A.  LDD2226  [2]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STS-2
 Probe Info  		N.A.  LDD0138  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA DM93 C46(2.73)  LDD0170  [3]
 LDCM0026  4SU-RNA+native RNA HEK-293T C46(3.93)  LDD0169  [3]
 LDCM0020  ARS-1620 HCC44 C115(1.27); C121(1.27)  LDD2171  [7]
 LDCM0632  CL-Sc Hep-G2 C46(0.74)  LDD2227  [2]
 LDCM0369  CL100 HEK-293T C229(0.68)  LDD1573  [4]
 LDCM0371  CL102 HEK-293T C46(1.01)  LDD1575  [4]
 LDCM0373  CL104 HEK-293T C229(0.79)  LDD1577  [4]
 LDCM0375  CL106 HEK-293T C46(0.85)  LDD1579  [4]
 LDCM0377  CL108 HEK-293T C229(1.12)  LDD1581  [4]
 LDCM0380  CL110 HEK-293T C46(1.02)  LDD1584  [4]
 LDCM0382  CL112 HEK-293T C229(0.83)  LDD1586  [4]
 LDCM0384  CL114 HEK-293T C46(0.97)  LDD1588  [4]
 LDCM0386  CL116 HEK-293T C229(0.81)  LDD1590  [4]
 LDCM0388  CL118 HEK-293T C46(1.09)  LDD1592  [4]
 LDCM0391  CL120 HEK-293T C229(0.74)  LDD1595  [4]
 LDCM0393  CL122 HEK-293T C46(0.99)  LDD1597  [4]
 LDCM0395  CL124 HEK-293T C229(0.75)  LDD1599  [4]
 LDCM0397  CL126 HEK-293T C46(1.11)  LDD1601  [4]
 LDCM0399  CL128 HEK-293T C229(0.73)  LDD1603  [4]
 LDCM0401  CL14 HEK-293T C46(1.04)  LDD1605  [4]
 LDCM0403  CL16 HEK-293T C229(0.82)  LDD1607  [4]
 LDCM0407  CL2 HEK-293T C46(0.94)  LDD1611  [4]
 LDCM0414  CL26 HEK-293T C46(0.95)  LDD1618  [4]
 LDCM0416  CL28 HEK-293T C229(0.75)  LDD1620  [4]
 LDCM0429  CL4 HEK-293T C229(0.95)  LDD1633  [4]
 LDCM0430  CL40 HEK-293T C229(0.69)  LDD1634  [4]
 LDCM0441  CL50 HEK-293T C46(1.13)  LDD1645  [4]
 LDCM0443  CL52 HEK-293T C229(1.24)  LDD1646  [4]
 LDCM0454  CL62 HEK-293T C46(1.08)  LDD1657  [4]
 LDCM0456  CL64 HEK-293T C229(0.88)  LDD1659  [4]
 LDCM0467  CL74 HEK-293T C46(1.00)  LDD1670  [4]
 LDCM0469  CL76 HEK-293T C229(0.70)  LDD1672  [4]
 LDCM0480  CL86 HEK-293T C46(1.11)  LDD1683  [4]
 LDCM0482  CL88 HEK-293T C229(0.86)  LDD1685  [4]
 LDCM0493  CL98 HEK-293T C46(0.88)  LDD1696  [4]
 LDCM0427  Fragment51 HEK-293T C46(1.03)  LDD1631  [4]
 LDCM0022  KB02 HEK-293T C229(0.94); C46(1.04)  LDD1492  [4]
 LDCM0023  KB03 HEK-293T C229(0.99); C46(0.96)  LDD1497  [4]
 LDCM0024  KB05 HEK-293T C229(0.94); C46(0.91)  LDD1502  [4]
 LDCM0021  THZ1 HCT 116 C115(1.27); C121(1.27)  LDD2173  [7]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
E3 SUMO-protein ligase PIAS4 (PIAS4) PIAS family Q8N2W9
E3 ubiquitin-protein ligase RNF4 (RNF4) . P78317
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Hypoxia-inducible factor 1-alpha (HIF1A) . Q16665
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein FAM9A (FAM9A) FAM9 family Q8IZU1
Troponin I, fast skeletal muscle (TNNI2) Troponin I family P48788
Peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PPARGC1A) . Q9UBK2

The Drug(s) Related To This Target

Approved
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Diethylstilbestrol Small molecular drug DB00255
Flavone Small molecular drug DB07776
Rimexolone Small molecular drug D0D2TN
Troglitazone Small molecular drug DB00197
Phase 4
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pregnenolone Small molecular drug D0B4RU
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
D-5519 . D0W8CW
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dexamethasone Palmitate Small molecular drug D07MME
Investigative
Click To Hide/Show 22 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1-cyclohexyl-n-{[1-(4-methylphenyl)-1h-indol-3-yl]Methyl}Methanamine Small molecular drug DB06833
7-bromo-6h-chromeno[4,3-b]Quinoline-3,9-diol Small molecular drug D00QDE
7-chloro-6h-chromeno[4,3-b]Quinoline-3,9-diol Small molecular drug D0W1YT
7-ethyl-6h-chromeno[4,3-b]Quinoline-3,9-diol Small molecular drug D07XJC
7-ethynyl-6h-chromeno[4,3-b]Quinoline-3,9-diol Small molecular drug D0RD6G
7-vinyl-6h-chromeno[4,3-b]Quinoline-3,9-diol Small molecular drug D0I1AF
Afimoxifene Small molecular drug DB04468
Biochanin A Small molecular drug D0S9YX
Chlordane Small molecular drug D01MFT
Daidzein Small molecular drug D0SY2M
Genistein Small molecular drug DB01645
Pmid17556356c1a Small molecular drug D0E7RI
Toxaphene Small molecular drug D0X6OV
Xct790 Small molecular drug D0ZB7Z
2-(4-hydroxy-phenyl)-4-vinyl-quinolin-6-ol . D0K7HR
4-bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol . D03CBX
4-chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol . D01TUB
4-ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol . D09FWS
4-ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol . D08SJL
Beta-naphthoflavone . DB06732
Ncx-1047 . D0LV7F
Tdt-044 . D06PFK
Discontinued
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Rofleponide Small molecular drug D0G9FP
Ad-121 . D06YFO
Gw-250495 . D01EDO
Pld-177 . D02WUW
Rpr-106541 . D09UGP
Steroid Hormone Conjugates . D03RZM

References

1 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
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 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
4 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
5 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
6 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
7 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.