General Information of Target

Target ID LDTP01660
Target Name Steroid hormone receptor ERR2 (ESRRB)
Gene Name ESRRB
Gene ID 2103
Synonyms
ERRB2; ESRL2; NR3B2; Steroid hormone receptor ERR2; ERR beta-2; Estrogen receptor-like 2; Estrogen-related receptor beta; ERR-beta; Nuclear receptor subfamily 3 group B member 2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSSDDRHLGSSCGSFIKTEPSSPSSGIDALSHHSPSGSSDASGGFGLALGTHANGLDSPP
MFAGAGLGGTPCRKSYEDCASGIMEDSAIKCEYMLNAIPKRLCLVCGDIASGYHYGVASC
EACKAFFKRTIQGNIEYSCPATNECEITKRRRKSCQACRFMKCLKVGMLKEGVRLDRVRG
GRQKYKRRLDSESSPYLSLQISPPAKKPLTKIVSYLLVAEPDKLYAMPPPGMPEGDIKAL
TTLCDLADRELVVIIGWAKHIPGFSSLSLGDQMSLLQSAWMEILILGIVYRSLPYDDKLV
YAEDYIMDEEHSRLAGLLELYRAILQLVRRYKKLKVEKEEFVTLKALALANSDSMYIEDL
EAVQKLQDLLHEALQDYELSQRHEEPWRTGKLLLTLPLLRQTAAKAVQHFYSVKLQGKVP
MHKLFLEMLEAKV
Target Type
Literature-reported
Target Bioclass
Transcription factor
Family
Nuclear hormone receptor family, NR3 subfamily
Subcellular location
Nucleus
Function
[Isoform 3]: Transcription factor that binds a canonical ESRRB recognition (ERRE) sequence 5'TCAAGGTCA-3' localized on promoter and enhancer of targets genes regulating their expression or their transcription activity. Plays a role, in a LIF-independent manner, in maintainance of self-renewal and pluripotency of embryonic and trophoblast stem cells through different signaling pathways including FGF signaling pathway and Wnt signaling pathways. Upon FGF signaling pathway activation, interacts with KDM1A by directly binding to enhancer site of ELF5 and EOMES and activating their transcription leading to self-renewal of trophoblast stem cells. Also regulates expression of multiple rod-specific genes and is required for survival of this cell type. Plays a role as transcription factor activator of GATA6, NR0B1, POU5F1 and PERM1. Plays a role as transcription factor repressor of NFE2L2 transcriptional activity and ESR1 transcriptional activity. During mitosis remains bound to a subset of interphase target genes, including pluripotency regulators, through the canonical ESRRB recognition (ERRE) sequence, leading to their transcriptional activation in early G1 phase. Can coassemble on structured DNA elements with other transcription factors like SOX2, POU5F1, KDM1A and NCOA3 to trigger ESRRB-dependent gene activation. This mechanism, in the case of SOX2 corecruitment prevents the embryonic stem cells (ESCs) to epiblast stem cells (EpiSC) transition through positive regulation of NR0B1 that inhibits the EpiSC transcriptional program. Also plays a role inner ear development by controlling expression of ion channels and transporters and in early placentation.; [Isoform 1]: Transcription factor that binds a canonical ESRRB recognition (ERRE) sequence 5'TCAAGGTCA-3' localized on promoter and enhancer of targets genes regulating their expression or their transcription activity. Positively regulates ESR1 transcriptional activity upon E2 stimulation.
TTD ID
T42025
Uniprot ID
O95718
DrugMap ID
TTKF0XS
Ensemble ID
ENST00000380887.7
HGNC ID
HGNC:3473
ChEMBL ID
CHEMBL3751

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C91(1.06)  LDD1573  [1]
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  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0369  CL100 HEK-293T C91(1.06)  LDD1573  [1]
 LDCM0372  CL103 HEK-293T C91(1.20)  LDD1576  [1]
 LDCM0373  CL104 HEK-293T C91(1.01)  LDD1577  [1]
 LDCM0376  CL107 HEK-293T C91(1.28)  LDD1580  [1]
 LDCM0377  CL108 HEK-293T C91(0.51)  LDD1581  [1]
 LDCM0381  CL111 HEK-293T C91(1.17)  LDD1585  [1]
 LDCM0382  CL112 HEK-293T C91(0.88)  LDD1586  [1]
 LDCM0385  CL115 HEK-293T C91(1.13)  LDD1589  [1]
 LDCM0386  CL116 HEK-293T C91(0.91)  LDD1590  [1]
 LDCM0389  CL119 HEK-293T C91(1.35)  LDD1593  [1]
 LDCM0391  CL120 HEK-293T C91(0.99)  LDD1595  [1]
 LDCM0394  CL123 HEK-293T C91(1.00)  LDD1598  [1]
 LDCM0395  CL124 HEK-293T C91(0.98)  LDD1599  [1]
 LDCM0398  CL127 HEK-293T C91(1.09)  LDD1602  [1]
 LDCM0399  CL128 HEK-293T C91(0.96)  LDD1603  [1]
 LDCM0402  CL15 HEK-293T C91(1.17)  LDD1606  [1]
 LDCM0403  CL16 HEK-293T C91(1.02)  LDD1607  [1]
 LDCM0415  CL27 HEK-293T C91(1.08)  LDD1619  [1]
 LDCM0416  CL28 HEK-293T C91(0.87)  LDD1620  [1]
 LDCM0418  CL3 HEK-293T C91(1.11)  LDD1622  [1]
 LDCM0428  CL39 HEK-293T C91(1.14)  LDD1632  [1]
 LDCM0429  CL4 HEK-293T C91(0.94)  LDD1633  [1]
 LDCM0430  CL40 HEK-293T C91(0.86)  LDD1634  [1]
 LDCM0443  CL52 HEK-293T C91(1.03)  LDD1646  [1]
 LDCM0455  CL63 HEK-293T C91(1.03)  LDD1658  [1]
 LDCM0456  CL64 HEK-293T C91(0.97)  LDD1659  [1]
 LDCM0469  CL76 HEK-293T C91(0.88)  LDD1672  [1]
 LDCM0481  CL87 HEK-293T C91(1.39)  LDD1684  [1]
 LDCM0482  CL88 HEK-293T C91(0.86)  LDD1685  [1]
 LDCM0494  CL99 HEK-293T C91(1.19)  LDD1697  [1]
 LDCM0495  E2913 HEK-293T C91(1.23)  LDD1698  [1]
 LDCM0468  Fragment33 HEK-293T C91(1.05)  LDD1671  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Diethylstilbestrol Small molecular drug DB00255
Flavone Small molecular drug DB07776
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Biochanin A Small molecular drug D0S9YX
Daidzein Small molecular drug D0SY2M
Dy131 Small molecular drug D06JPQ
Genistein Small molecular drug DB01645

References

1 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
2 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.