| + |
afimoxifene | down-regulates activity 
chemical inhibition
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258596 |
|
|
in vitro |
|
| pmid |
sentence |
| 9048584 |
In total 37 substances were tested for both ER subtypes (Fig. 3 and Table 1). In Fig. 3 several examples of typical competitor curves obtained are shown. In all cases monophasic curves were obtained for compounds with significant affinity. . The present study is the first in which the ligand binding properties of both ER subtypes are measured separately, and caution is needed when comparing RBAs from this study with the previous studies involving mixtures of ER subtypes. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
estriol | up-regulates activity 
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258585 |
|
|
in vitro |
|
| pmid |
sentence |
| 9048584 |
In total 37 substances were tested for both ER subtypes (Fig. 3 and Table 1). In Fig. 3 several examples of typical competitor curves obtained are shown. In all cases monophasic curves were obtained for compounds with significant affinity. . The present study is the first in which the ligand binding properties of both ER subtypes are measured separately, and caution is needed when comparing RBAs from this study with the previous studies involving mixtures of ER subtypes. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
perfluorooctane-1-sulfonic acid | up-regulates activity
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268763 |
|
|
in vitro |
|
| pmid |
sentence |
| 23764977 |
Seven PFCs [perfluorohexane sulfonate (PFHxS), perfluorooctane sulfonate (PFOS), perfluorooctanoate (PFOA), perfluorononanoate (PFNA), perfluorodecanoate (PFDA), perfluoroundecanoate (PFUnA), and perfluorododecanoate (PFDoA)] were analyzed in vitro for their potential to affect estrogen receptor (ER) and androgen receptor (AR) transactivity as well as aromatase enzyme activity. The PFCs were assessed as single compounds and in an equimolar mixture. PFHxS, PFOS and PFOA significantly induced the ER transactivity, whereas PFHxS, PFOS, PFOA, PFNA and PFDA significantly antagonized the AR activity in a concentration-dependent manner. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
fulvestrant | down-regulates activity
chemical inhibition
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259304 |
|
|
Homo sapiens |
Breast Cancer Cell |
| pmid |
sentence |
| 12113237 |
Fulvestrant (Faslodex, formerly ICI 182,780) is a potent steroidal antiestrogen that mediates its effects by estrogen receptor downregulation. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
perfluorohexanesulfonic acid | up-regulates activity
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268764 |
|
|
in vitro |
|
| pmid |
sentence |
| 23764977 |
Seven PFCs [perfluorohexane sulfonate (PFHxS), perfluorooctane sulfonate (PFOS), perfluorooctanoate (PFOA), perfluorononanoate (PFNA), perfluorodecanoate (PFDA), perfluoroundecanoate (PFUnA), and perfluorododecanoate (PFDoA)] were analyzed in vitro for their potential to affect estrogen receptor (ER) and androgen receptor (AR) transactivity as well as aromatase enzyme activity. The PFCs were assessed as single compounds and in an equimolar mixture. PFHxS, PFOS and PFOA significantly induced the ER transactivity, whereas PFHxS, PFOS, PFOA, PFNA and PFDA significantly antagonized the AR activity in a concentration-dependent manner. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
ESR2 | up-regulates quantity by expression 
transcriptional regulation
|
TGFA |
0.262 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253944 |
|
|
Homo sapiens |
Breast Cancer Cell Line |
| pmid |
sentence |
| 11517191 |
ER beta and ER alpha induced the expression of several endogenous genes such as pS2, TGF alpha, or the cyclin kinase inhibitor p21 but, in contrast to ER alpha, ER beta was unable to regulate c-myc proto-oncogene expression |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ESR2 | up-regulates quantity by expression
transcriptional regulation
|
OXT |
0.489 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268547 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 6153132 |
The human and rat OT promoters could be stimulated by the ligand-activated estrogen receptors ERalpha and ERbeta, the thyroid hormone receptor THRapha, and the retinoic acid receptors RARalpha and RARbeta in a variety of cells (3, 477, 478). However, it is important to note that these results were obtained from cotransfection experiments in cell lines, i.e., under nonphysiological circumstances. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Oxytocin signaling |
| + |
ESR2 | down-regulates quantity by repression 
transcriptional regulation
|
SCN11A |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253475 |
|
|
Mus musculus |
Neuron |
| pmid |
sentence |
| 22169964 |
17β-Estradiol regulates the gene expression of voltage-gated sodium channels. . In this study, we investigate the mRNA expressions of Nav channel subtypes mediated differentially by the ERs in the DRGs of wild-type (WT) and estrogen receptor knockout (αERKO and βERKO) mice. In the present study, by means of quantitative real-time PCR, we found that the expressions of Nav1.1, Nav1.7, Nav1.8, and Nav1.9 subtypes were elevated in αERKO and βERKO mice |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| Tissue: |
Spinal Ganglion |
| + |
ESR1 | up-regulates
binding
|
ESR2 |
0.506 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-64427 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 10022879 |
It was recently shown that er? And er? Could form a heterodimer complex both in vitro and in vivo |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Oxytocin signaling |
| + |
dutasteride | up-regulates
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-191445 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
biphenyl-4,4'-diol | up-regulates activity
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268741 |
|
|
in vitro |
|
| pmid |
sentence |
| 9751507 |
Bisphenol A is an equally strong agonist for ERα as for ERβ, and the same is true for 4,4′-biphenol, which differs from bisphenol A in that it lacks the propane group between the phenolic rings. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
estrone | up-regulates activity
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258583 |
|
|
in vitro |
|
| pmid |
sentence |
| 9048584 |
In total 37 substances were tested for both ER subtypes (Fig. 3 and Table 1). In Fig. 3 several examples of typical competitor curves obtained are shown. In all cases monophasic curves were obtained for compounds with significant affinity. . The present study is the first in which the ligand binding properties of both ER subtypes are measured separately, and caution is needed when comparing RBAs from this study with the previous studies involving mixtures of ER subtypes. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
ESR2 | up-regulates quantity by expression
transcriptional regulation
|
TFF1 |
0.359 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253939 |
|
|
Homo sapiens |
Breast Cancer Cell Line |
| pmid |
sentence |
| 11517191 |
ER beta and ER alpha induced the expression of several endogenous genes such as pS2, TGF alpha, or the cyclin kinase inhibitor p21 but, in contrast to ER alpha, ER beta was unable to regulate c-myc proto-oncogene expression |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ESR2 | down-regulates quantity by repression
transcriptional regulation
|
SCN9A |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253473 |
|
|
Mus musculus |
Neuron |
| pmid |
sentence |
| 22169964 |
17β-Estradiol regulates the gene expression of voltage-gated sodium channels. . In this study, we investigate the mRNA expressions of Nav channel subtypes mediated differentially by the ERs in the DRGs of wild-type (WT) and estrogen receptor knockout (αERKO and βERKO) mice. In the present study, by means of quantitative real-time PCR, we found that the expressions of Nav1.1, Nav1.7, Nav1.8, and Nav1.9 subtypes were elevated in αERKO and βERKO mice |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| Tissue: |
Spinal Ganglion |
| + |
tamoxifen citrate | down-regulates activity
chemical inhibition
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259300 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 20512796 |
Estrogen receptor-alpha (ER) antagonists have been widely used for breast cancer therapy. Despite initial responsiveness, hormone-sensitive ER-positive cancer cells eventually develop resistance to ER antagonists. It has been shown that in most of these resistant tumor cells, the ER is expressed and continues to regulate tumor growth. Recent studies indicate that tamoxifen initially acts as an antagonist, but later functions as an ER agonist, promoting tumor growth. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
tamoxifen | down-regulates activity
chemical inhibition
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258588 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 20512796 |
Estrogen receptor-alpha (ER) antagonists have been widely used for breast cancer therapy. Despite initial responsiveness, hormone-sensitive ER-positive cancer cells eventually develop resistance to ER antagonists. It has been shown that in most of these resistant tumor cells, the ER is expressed and continues to regulate tumor growth. Recent studies indicate that tamoxifen initially acts as an antagonist, but later functions as an ER agonist, promoting tumor growth. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
17beta-estradiol | up-regulates
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-154663 |
|
|
Homo sapiens |
Breast Cancer Cell |
| pmid |
sentence |
| 17478088 |
Oestrogen receptors (er)alpha and beta modify the expression of genes involved in cell growth, proliferation and differentiation through binding to oestrogen response elements (eres) located in a number of gene promoters. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ESR2 | up-regulates quantity by expression
transcriptional regulation
|
CDKN1A |
0.295 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253943 |
|
|
Homo sapiens |
Breast Cancer Cell Line |
| pmid |
sentence |
| 11517191 |
ER beta and ER alpha induced the expression of several endogenous genes such as pS2, TGF alpha, or the cyclin kinase inhibitor p21 but, in contrast to ER alpha, ER beta was unable to regulate c-myc proto-oncogene expression |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
perfluorooctanoic acid | up-regulates activity
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268765 |
|
|
in vitro |
|
| pmid |
sentence |
| 23764977 |
Seven PFCs [perfluorohexane sulfonate (PFHxS), perfluorooctane sulfonate (PFOS), perfluorooctanoate (PFOA), perfluorononanoate (PFNA), perfluorodecanoate (PFDA), perfluoroundecanoate (PFUnA), and perfluorododecanoate (PFDoA)] were analyzed in vitro for their potential to affect estrogen receptor (ER) and androgen receptor (AR) transactivity as well as aromatase enzyme activity. The PFCs were assessed as single compounds and in an equimolar mixture. PFHxS, PFOS and PFOA significantly induced the ER transactivity, whereas PFHxS, PFOS, PFOA, PFNA and PFDA significantly antagonized the AR activity in a concentration-dependent manner. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
estramustine | up-regulates activity
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259299 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 14755680 |
A variety of new estrogenic/anti‐estrogenic/selective estrogen receptor modulator (SERM)‐like compounds, including 2‐methoxyestradiol, genistein, resveratrol, licochalcone, Raloxifene, ICI 182,780, and estramustine are being evaluated for their potential in the next generation of PCa therapies. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
NR0B2 | down-regulates quantity by repression
transcriptional regulation
|
ESR2 |
0.609 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-74291 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 10648597 |
These novel insights provide a mechanistic explanation for the inhibitory role of shp in nuclear receptor signaling, and they may explain how shp functions as a negative coregulator or corepressor for ligand-activated receptors, a novel and unique function for an orphan nuclear receptor. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ESR2 | down-regulates quantity by repression
transcriptional regulation
|
SCN10A |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253474 |
|
|
Mus musculus |
Neuron |
| pmid |
sentence |
| 22169964 |
17β-Estradiol regulates the gene expression of voltage-gated sodium channels. . In this study, we investigate the mRNA expressions of Nav channel subtypes mediated differentially by the ERs in the DRGs of wild-type (WT) and estrogen receptor knockout (αERKO and βERKO) mice. In the present study, by means of quantitative real-time PCR, we found that the expressions of Nav1.1, Nav1.7, Nav1.8, and Nav1.9 subtypes were elevated in αERKO and βERKO mice |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| Tissue: |
Spinal Ganglion |
| + |
17beta-estradiol | up-regulates activity
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258592 |
|
|
in vitro |
|
| pmid |
sentence |
| 9048584 |
In total 37 substances were tested for both ER subtypes (Fig. 3 and Table 1). In Fig. 3 several examples of typical competitor curves obtained are shown. In all cases monophasic curves were obtained for compounds with significant affinity. . The present study is the first in which the ligand binding properties of both ER subtypes are measured separately, and caution is needed when comparing RBAs from this study with the previous studies involving mixtures of ER subtypes. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
bisphenol A | up-regulates activity
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268739 |
|
|
in vitro |
|
| pmid |
sentence |
| 9751507 |
Bisphenol A is an equally strong agonist for ERα as for ERβ, and the same is true for 4,4′-biphenol, which differs from bisphenol A in that it lacks the propane group between the phenolic rings. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
ESR2 | up-regulates quantity by expression
transcriptional regulation
|
CRH |
0.396 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268722 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 8408641 |
Evidence of direct estrogenic regulation of human corticotropin-releasing hormone gene expression. Potential implications for the sexual dimophism of the stress response and immune/inflammatory reaction.|Gel retardation and immunoprecipitation demonstrated specific association between the perfect half-palindromic EREs of hCRH gene and the DNA binding domain of hER in vitro. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Hypothalamus |
| + |
ESR2 | down-regulates quantity by repression
transcriptional regulation
|
SCN1A |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253472 |
|
|
Mus musculus |
Neuron |
| pmid |
sentence |
| 22169964 |
17β-Estradiol regulates the gene expression of voltage-gated sodium channels. . In this study, we investigate the mRNA expressions of Nav channel subtypes mediated differentially by the ERs in the DRGs of wild-type (WT) and estrogen receptor knockout (αERKO and βERKO) mice. In the present study, by means of quantitative real-time PCR, we found that the expressions of Nav1.1, Nav1.7, Nav1.8, and Nav1.9 subtypes were elevated in αERKO and βERKO mice |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| Tissue: |
Spinal Ganglion |
| + |
diethylstilbestrol | up-regulates activity
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258597 |
|
|
in vitro |
|
| pmid |
sentence |
| 9048584 |
In total 37 substances were tested for both ER subtypes (Fig. 3 and Table 1). In Fig. 3 several examples of typical competitor curves obtained are shown. In all cases monophasic curves were obtained for compounds with significant affinity. . The present study is the first in which the ligand binding properties of both ER subtypes are measured separately, and caution is needed when comparing RBAs from this study with the previous studies involving mixtures of ER subtypes. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
genistein | up-regulates activity
chemical activation
|
ESR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258599 |
|
|
in vitro |
|
| pmid |
sentence |
| 9048584 |
In total 37 substances were tested for both ER subtypes (Fig. 3 and Table 1). In Fig. 3 several examples of typical competitor curves obtained are shown. In all cases monophasic curves were obtained for compounds with significant affinity. . The present study is the first in which the ligand binding properties of both ER subtypes are measured separately, and caution is needed when comparing RBAs from this study with the previous studies involving mixtures of ER subtypes. |
|
| Publications: |
1 |
Organism: |
In Vitro |
3.0
ESR2
- 
- 