General Information of the Protein
Protein ID
PT02640
Protein Name
Steroid hormone receptor ERR2
Secondarily
Protein Name
ERR beta-2
Estrogen receptor-like 2
Estrogen-related receptor beta
Nuclear receptor subfamily 3 group B member 2
Gene Name
ESRRB
Secondarily
Gene Name
ERRB2
ESRL2
NR3B2
Sequence
MSSDDRHLGSSCGSFIKTEPSSPSSGIDALSHHSPSGSSDASGGFGLALGTHANGLDSPPMFAGAGLGGTPCRKSYEDCASGIMEDSAIKCEYMLNAIPKRLCLVCGDIASGYHYGVASCEACKAFFKRTIQGNIEYSCPATNECEITKRRRKSCQACRFMKCLKVGMLKEGVRLDRVRGGRQKYKRRLDSESSPYLSLQISPPAKKPLTKIVSYLLVAEPDKLYAMPPPGMPEGDIKALTTLCDLADRELVVIIGWAKHIPGFSSLSLGDQMSLLQSAWMEILILGIVYRSLPYDDKLVYAEDYIMDEEHSRLAGLLELYRAILQLVRRYKKLKVEKEEFVTLKALALANSDSMYIEDLEAVQKLQDLLHEALQDYELSQRHEEPWRTGKLLLTLPLLRQTAAKAVQHFYSVKLQGKVPMHKLFLEMLEAKV
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Organism
Homo sapiens, Human
Protein Classification
Transcription factor
>
Nuclear receptor
>
Nuclear hormone receptor subfamily 3
>
Nuclear hormone receptor subfamily 3 group B
>
Nuclear hormone receptor subfamily 3 group B member 2
Function
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 (PubMed:17920186, PubMed:19755138). 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 (By similarity). Plays a role as transcription factor activator of GATA6, NR0B1, POU5F1 and PERM1 (PubMed:23836911). Plays a role as transcription factor repressor of NFE2L2 transcriptional activity and ESR1 transcriptional activity (PubMed:17920186, PubMed:19755138). 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 (By similarity).
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Uniprot ID
Primary ID:
O95718

Secondarily ID:
A2VDJ2
B6ZGU4
Q5F0P7
Q5F0P8
Q9HCB4
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HGNC ID
HGNC:3473
Subcellular Location
Nucleus
Cytoplasm
Chromosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000044 , CV-1
Compound ID Compound Name Compound Formula
CP0391805
[4-[(E)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-3-methyl-2-phenylbut-1-enyl]phenyl] acetate
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C29H33NO3
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0410156
methyl (Z)-5-[4-[2-(dimethylamino)ethoxy]phenyl]-5-(4-hydroxyphenyl)-2-methyl-4-phenylpent-4-enoate
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C29H33NO4
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0411193
4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-3-methyl-2-phenylbut-1-enyl]phenol
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C27H31NO2
 1
1
IC50 = 210 nM
   TI
   LI
   LO
   TS
CP0526262
methyl 5,5-bis(4-hydroxyphenyl)-2-methyl-4-phenylpent-4-enoate
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C25H24O4
 1
1
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0481182
methyl (Z)-5-[4-[2-(dimethylamino)ethoxy]phenyl]-5-(4-hydroxyphenyl)-4-phenylpent-4-enoate
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C28H31NO4
 1
1
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0481181
[4-[(E)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-5-hydroxy-4-methyl-2-phenylpent-1-enyl]phenyl] acetate
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C30H35NO4
 1
1
IC50 = 550 nM
   TI
   LI
   LO
   TS
CP0454775
methyl 5,5-bis(4-hydroxyphenyl)-4-phenylpent-4-enoate
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C24H22O4
 1
1
IC50 = 600 nM
   TI
   LI
   LO
   TS
CP0648741
4-Hydroxytamoxifen
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C26H29NO2
 1
1
IC50 = 650 nM
   TI
   LI
   LO
   TS
CP0454777
4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-4-methyl-2-phenylpent-1-enyl]phenol
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C28H33NO2
 1
1
IC50 = 750 nM
   TI
   LI
   LO
   TS
CP0454776
[4-[(E)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenyl] acetate
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C29H33NO4
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0410155
4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-5-hydroxy-4-methyl-2-phenylpent-1-enyl]phenol
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C28H33NO3
 1
1
IC50 = 2250 nM
   TI
   LI
   LO
   TS
CP0176271
4-[(1Z)-1-{4-[2-(dimethylamino)ethoxy]phenyl}-5-hydroxy-2-phenylpent-1-en-1-yl]phenol
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C27H31NO3
 1
1
IC50 = 3500 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0006292
(1S,10R,11S,14S,15S)-15-methyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2,4,6-triene-5,14-diol
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C18H24O2
 2
1 IC50 = 3.2 nM
2 IC50 = 8.7 nM
CP0648741
4-Hydroxytamoxifen
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C26H29NO2
 1
1 IC50 = 886 nM
CP0176271
4-[(1Z)-1-{4-[2-(dimethylamino)ethoxy]phenyl}-5-hydroxy-2-phenylpent-1-en-1-yl]phenol
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C27H31NO3
 1
1 IC50 > 10000 nM
Clinical Information about the Protein
Target 1 ( Estrogen-related receptor-beta (ESRRB) )
Target Type Literature-reported Target