Search results for ESR1

Showing 22 results out of 159

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Protein (4 results from a total of 16)

Identifier: R-HSA-9020968
Species: Homo sapiens
Compartment: cytosol
Primary external reference: UniProt: ESR1: P03372
Identifier: R-HSA-446168
Species: Homo sapiens
Compartment: nucleoplasm
Primary external reference: UniProt: ESR1: P03372
Identifier: R-HSA-9021057
Species: Homo sapiens
Compartment: plasma membrane
Primary external reference: UniProt: ESR1: P03372
Identifier: R-HSA-9020974
Species: Homo sapiens
Compartment: cytosol
Primary external reference: UniProt: ESR1: P03372

Interactor (1 results from a total of 1)

Identifier: P03372-1
Species: Homo sapiens
Primary external reference: UniProt: P03372-1

Reaction (4 results from a total of 85)

Identifier: R-HSA-9716947
Species: Homo sapiens
Compartment: nucleoplasm
Estrogen receptor alpha (ERα, NR3A1, nuclear receptor subfamily 3 group A member 1), encoded by the ESR1 gene, is a nuclear hormone receptor that is activated by the sex hormone estrogen. ESR1 can mediate the physiological development and function of various organ systems, including the reproductive, central nervous, skeletal, and cardiovascular systems. Accordingly, ESR1 is widely expressed throughout the body.

Synthetic nonsteroidal estrogen agonists are used to treat a variety of gynecological disorders (Stauffer et al. 2000, Sasson 1991, Kuiper et al. 1997). Diethylstilbestrol was previously used in the prevention of miscarriage or premature delivery but later only used in the treatment of prostate or breast cancer. Ethinylestradiol, when combined with progestins, is mainly used as a contraceptive and for certain menopausal conditions.

Tamoxifen has mixed estrogenic and antiestrogenic activity, dependent on tissue type. For instance, tamoxifen has predominantly antiestrogenic effects in breast tissue (Wang et al. 2004) but predominantly estrogenic effects in the uterus and liver. Tamoxifen was indicated to treat estrogen receptor positive metastatic breast cancer in adults but has since been superceded by aromatase inhibitors such as anastrozole (Howell et al. 2005). A beneficial side effect of tamoxifen is that it prevents osteoporosis by acting as an agonist in bone cells (Kassem 1997). Tibolone is an estrogen receptor agonist with a preference for ESR1 (Escande et al. 2009). It is indicated for the relief of post-menopausal symptoms and for the prevention of osteoporosis.
Identifier: R-HSA-9716913
Species: Homo sapiens
Compartment: nucleoplasm
Estrogen receptor alpha (ERα, NR3A1, nuclear receptor subfamily 3 group A member 1), encoded by the ESR1 gene, is a nuclear hormone receptor that is activated by the sex hormone estrogen. ESR1 can mediate the physiological development and function of various organ systems, including the reproductive, central nervous, skeletal, and cardiovascular systems (Kassem 1997). Accordingly, ESR1 is widely expressed throughout the body.

Antiestrogens (aka estrogen antagonists or estrogen blockers) are a class of drugs which prevent endogenous estrogens like estradiol from mediating their biological effects in the body. They act by blocking the estrogen receptor (selective estrogen receptor modulators (SERMs)) or inhibiting/suppressing estrogen production (selective estrogen receptor downregulators (SERDs)) (Kuiper et al. 1997, Sasson 1991, Fan et al. 2007). SERMs include tamoxifen (Wang et al. 2004), clomifene (Kurosawa et al. 2010), bazedoxifene (Toniti et al. 2011) and raloxifene (Schafer et al. 1999), and a SERD drug is fulvestrant (Schmidt et al. 2003).

Bazedoxifene is used in the treatment of moderate to severe vasomotor symptoms associated with menopause and for postmenopausal osteoporosis (Genant 2011, Rossini et al. 2013). Fulvestrant used to treat hormone receptor (HR)-positive metastatic breast cancer in postmenopausal women (Lee et al. 2017, Lei et al. 2020). Clomiphene, is a medication used to treat infertility in women who do not ovulate, including those with polycystic ovary syndrome (Hughes et al. 2010). Raloxifene medication used to prevent and treat osteoporosis in postmenopausal women and those on glucocorticoids. It is also used to reduce the risk of breast cancer in those at high risk (Scott et al. 1999). Tamoxifen is used for the treatment of both early and advanced estrogen receptor-positive (ER-positive or ER+) breast cancer in pre- and postmenopausal women (Jordan 2021). Tamoxifen is also used for ovulation induction to treat infertility in women with anovulatory disorders.
Identifier: R-HSA-8937369
Species: Homo sapiens
Compartment: nucleoplasm
ATPase family AAA domain-containing protein 2 (ATAD2 aka ANCCA) is a highly conserved protein primarily located in the cell nucleus. Its protein structure consists of two AAA domains and one bromodomain, indicating roles related to genome regulation, such as acting on chromatin structure and function (Caron et al. 2010, Magnani & Lupien 2014). ATAD2 is highly expressed in multiple cancers (Krakstad et al. 2015, Ciro et al. 2009, ) and is a strong predictor of rapid mortality in lung and breast cancers sufferers (Caron et al. 2010). Additionally, ATAD2 functions as a co-activator of the estrogen receptor (ESR1) and the androgen receptor (Zou et al. 2009), implicating it as an oncogenic protein in hormone-related cancers such as breast cancer and prostate cancer (Zou et al. 2007). This reaction shows ATAD2 binding to ESR1.
Identifier: R-HSA-8931981
Species: Homo sapiens
Compartment: nucleoplasm
The RUNX1:CBFB complex binds the estrogen receptor alpha (ESR1). The interaction between RUNX1 and ESR1 is significantly enhanced upon ESR1 activation by estrogens (Stender et al. 2010).

DNA Sequence (1 results from a total of 1)

Identifier: R-HSA-8864383
Species: Homo sapiens
Compartment: nucleoplasm
Primary external reference: ENSEMBL: ENSEMBL:ENSG00000091831

Complex (4 results from a total of 39)

Identifier: R-HSA-1254381
Species: Homo sapiens
Compartment: nucleoplasm
Identifier: R-HSA-1254384
Species: Homo sapiens
Compartment: nucleoplasm
Identifier: R-HSA-9008284
Species: Homo sapiens
Compartment: nucleoplasm
Identifier: R-HSA-9023832
Species: Homo sapiens
Compartment: nucleoplasm

Set (4 results from a total of 5)

Identifier: R-ALL-9716906
Compartment: nucleoplasm
Identifier: R-ALL-9716925
Compartment: nucleoplasm
Identifier: R-HSA-6783282
Species: Homo sapiens
Compartment: nucleoplasm
Identifier: R-HSA-9023865
Species: Homo sapiens
Compartment: nucleoplasm

Pathway (4 results from a total of 12)

Identifier: R-HSA-9018519
Species: Homo sapiens
Estrogens mediate their transcriptional effects through interaction with the estrogen receptors, ESR1 (also known as ER alpha) and ESR2 (ER beta). ESR1 and ESR2 share overlapping but distinct functions, with ESR1 playing the primary role in transcriptional activation in most cell types (Hah and Krauss, 2014; Haldosén et al, 2014. The receptors function as ligand-dependent dimers and can activate target genes either through direct binding to an estrogen responsive element (ERE) in the target gene promoter, or indirectly through interaction with another DNA-binding protein such as RUNX1, SP1, AP1 or NF-kappa beta (reviewed in Bai and Gust, 2009; Hah and Krause, 2014). Binding of estrogen receptors to the DNA promotes the assembly of higher order transcriptional complexes containing methyltransferases, histone acetyltransferases and other transcriptional activators, which promote transcription by establishing active chromatin marks and by recruiting general transcription factors and RNA polymerase II. ESR1- and estrogen-dependent recruitment of up to hundreds of coregulators has been demonstrated by varied co-immunoprecipitation and proteomic approaches (Kittler et al, 2013; Mohammed et al, 2013; Foulds et al, 2013; Mohammed et al, 2015; Liu et al, 2014; reviewed in Magnani and Lupien, 2014; Arnal, 2017). In some circumstances, ligand-bound receptors can also promote the assembly of a repression complex at a target gene, and in some cases, heterodimers of ESR1 and ESR2 serve as repressors of ESR1-mediated target gene activation (reviewed in Hah and Kraus, 2014; Arnal et al, 2017). Phosphorylation of the estrogen receptor also modulates its activity, and provides cross-talk between nuclear estrogen-dependent signaling and non-genomic estrogen signaling from the plasma membrane (reviewed in Anbalagan and Rowan, 2015; Halodsèn et al, 2014; Schwartz et al, 2016)

A number of recent genome wide studies highlight the breadth of the transcriptional response to estrogen. The number of predicted estrogen-dependent target genes ranges from a couple of hundred (based on microarray studies) to upwards of 10000, based on ChIP-chip or ChIP-seq (Cheung and Kraus, 2010; Kinnis and Kraus, 2008; Lin et al, 2004; Welboren et al, 2009; Ikeda et al, 2015; Lin et al, 2007; Carroll et al, 2006). Many of these predicted sites may not represent transcriptionally productive binding events, however. A study examining ESR1 binding by ChIP-seq in 20 primary breast cancers identified a core of 484 ESR-binding events that were conserved in at least 75% of ER+ tumors, which may represent a more realistic estimate (Ross-Innes et al, 2012). These studies also highlight the long-range effect of estrogen receptor-binding, with distal enhancer or promoter elements regulating the expression of many target genes, often through looping or other higher order chromatin structures (Kittler et al, 2013; reviewed in Dietz and Carroll, 2008; Liu and Cheung, 2014; Magnani and Lupien, 2014). Transcription from a number of estrogen-responsive target genes also appears to be primed by the binding of pioneering transcription factors such as FOXA1, GATA3, PBX1 among others. These factors bind to heterochromatin by virtue of their winged helix domains and promote chromatin opening, allowing subsequent recruitment of other transcription factors (reviewed in Zaret and Carroll, 2011; Fiorito et al, 2013; Arnal et al, 2017; Magnani et al, 2011)
Identifier: R-HSA-8931987
Species: Homo sapiens
The RUNX1:CBFB complex can associate with the activated estrogen receptor alpha (ESR1) through direct interaction between RUNX1 and ESR1. The RUNX1:CBFB complex is thus involved in transcriptional regulation of estrogen responsive genes, including GPAM, KCTD6 and AXIN1 (Stender et al. 2010). High GPAM expression correlates with better overall survival in breast cancer (Brockmoller et al. 2012).
Identifier: R-HSA-9634597
Species: Homo sapiens
GPER1 (also known as GPR30) is an orphan G-protein coupled receptor that has been suggested to act as an alternate estrogen receptor (Revankar et al, 2005; Filardo et al, 2007; reviewed in Prossnitz and Barton, 2011; Gaudet et al, 2015). In support of this, a number of studies have shown that GPER1 stimulates MAPK and cAMP activation in response to estrogen in ESR1 negative breast cancer cells. Similar to classical ESR1-mediated signaling, this estrogen-responsive GPER1 is suggested to act through G beta gamma and to involve EGFR transactivation (Filardo et al, 2000; Filardo et al, 2002; reviewed in Filardo and Thomas, 2012).
Identifier: R-HSA-8939256
Species: Homo sapiens
Compartment: nucleoplasm
The RUNX1:CBFB complex directly regulates transcription of at least two components of WNT signaling. In association with its co-factor FOXP3, the RUNX1:CBFB complex stimulates transcription of the RSPO3 gene, encoding a WNT ligand that is implicated as a breast cancer oncogene (Recouvreux et al. 2016). In association with the activated estrogen receptor alpha (ESR1), the RUNX1:CBFB complex stimulates the expression of AXIN1, which functions as a regulator of WNT signaling (Stender et al. 2010).
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