| Tchem | Estrogen-related receptor gamma |
Orphan receptor that acts as transcription activator in the absence of bound ligand. Binds specifically to an estrogen response element and activates reporter genes controlled by estrogen response elements (By similarity). Induces the expression of PERM1 in the skeletal muscle.
This gene encodes a member of the estrogen receptor-related receptor (ESRR) family, which belongs to the nuclear hormone receptor superfamily. All members of the ESRR family share an almost identical DNA binding domain, which is composed of two C4-type zinc finger motifs. The ESRR members are orphan nuclear receptors; they bind to the estrogen response element and steroidogenic factor 1 response element, and activate genes controlled by both response elements in the absence of any ligands. The ESRR family is closely related to the estrogen receptor (ER) family. They share target genes, co-regulators and promoters, and by targeting the same set of genes, the ESRRs seem to interfere with the ER-mediated estrogen response in various ways. It has been reported that the family member encoded by this gene functions as a transcriptional activator of DNA cytosine-5-methyltransferases 1 (Dnmt1) expression by direct binding to its response elements in the DNMT1 promoters, modulates cell proliferation and estrogen signaling in breast cancer, and negatively regulates bone morphogenetic protein 2-induced osteoblast differentiation and bone formation. Multiple alternatively spliced transcript variants have been identified, which mainly differ at the 5' end and some of which encode protein isoforms differing in the N-terminal region. [provided by RefSeq, Aug 2011]
This gene encodes a member of the estrogen receptor-related receptor (ESRR) family, which belongs to the nuclear hormone receptor superfamily. All members of the ESRR family share an almost identical DNA binding domain, which is composed of two C4-type zinc finger motifs. The ESRR members are orphan nuclear receptors; they bind to the estrogen response element and steroidogenic factor 1 response element, and activate genes controlled by both response elements in the absence of any ligands. The ESRR family is closely related to the estrogen receptor (ER) family. They share target genes, co-regulators and promoters, and by targeting the same set of genes, the ESRRs seem to interfere with the ER-mediated estrogen response in various ways. It has been reported that the family member encoded by this gene functions as a transcriptional activator of DNA cytosine-5-methyltransferases 1 (Dnmt1) expression by direct binding to its response elements in the DNMT1 promoters, modulates cell proliferation and estrogen signaling in breast cancer, and negatively regulates bone morphogenetic protein 2-induced osteoblast differentiation and bone formation. Multiple alternatively spliced transcript variants have been identified, which mainly differ at the 5' end and some of which encode protein isoforms differing in the N-terminal region. [provided by RefSeq, Aug 2011]
Comments
| Disease | Target Count | P-value |
|---|---|---|
| atypical teratoid / rhabdoid tumor | 4971 | 7.7e-09 |
| psoriasis | 6514 | 1.7e-07 |
| lung cancer | 4607 | 6.7e-05 |
| pancreatic cancer | 2322 | 1.6e-04 |
| interstitial cystitis | 2237 | 2.5e-04 |
| glioblastoma | 5635 | 8.8e-04 |
| Astrocytoma, Pilocytic | 3006 | 1.2e-03 |
| nephrosclerosis | 314 | 5.6e-03 |
| fascioscapulohumeral muscular dystrophy | 98 | 5.8e-03 |
| adult high grade glioma | 3701 | 6.4e-03 |
| astrocytic glioma | 2530 | 8.7e-03 |
| intraductal papillary-mucinous neoplasm (IPMN) | 3204 | 9.5e-03 |
| dermatomyositis | 941 | 1.1e-02 |
| cutaneous lupus erythematosus | 1016 | 1.1e-02 |
| ependymoma | 4559 | 2.0e-02 |
| medulloblastoma, large-cell | 6086 | 2.2e-02 |
| intraductal papillary-mucinous adenoma (IPMA) | 2872 | 3.1e-02 |
| group 3 medulloblastoma | 4002 | 3.8e-02 |
| ductal carcinoma in situ | 1686 | 3.9e-02 |
| gastric carcinoma | 781 | 4.4e-02 |
| Disease | Target Count | Z-score | Confidence |
|---|---|---|---|
| Eye and adnexa disease | 17 | 0.0 | 0.9 |
| Heart disease | 288 | 0.0 | 2.7 |
| Mental Depression | 325 | 0.0 | 0.7 |
| substance-related disorder | 156 | 0.0 | 0.9 |
| Disease | log2 FC | p |
|---|---|---|
| lung cancer | 2.300 | 6.7e-05 |
| adult high grade glioma | -1.600 | 6.4e-03 |
| astrocytic glioma | -1.800 | 8.7e-03 |
| Astrocytoma, Pilocytic | -1.300 | 1.2e-03 |
| atypical teratoid / rhabdoid tumor | -3.900 | 7.7e-09 |
| cutaneous lupus erythematosus | -1.100 | 1.1e-02 |
| dermatomyositis | 1.300 | 1.1e-02 |
| ductal carcinoma in situ | 1.400 | 3.9e-02 |
| ependymoma | -1.700 | 2.0e-02 |
| fascioscapulohumeral muscular dystrophy | 1.060 | 5.8e-03 |
| gastric carcinoma | -4.800 | 4.4e-02 |
| glioblastoma | -1.200 | 8.8e-04 |
| group 3 medulloblastoma | 1.400 | 3.8e-02 |
| interstitial cystitis | -2.000 | 2.5e-04 |
| intraductal papillary-mucinous adenoma (... | -1.200 | 3.1e-02 |
| intraductal papillary-mucinous neoplasm ... | -2.200 | 9.5e-03 |
| medulloblastoma, large-cell | 1.200 | 2.2e-02 |
| nephrosclerosis | -1.562 | 5.6e-03 |
| pancreatic cancer | -1.400 | 1.6e-04 |
| psoriasis | -1.100 | 1.7e-07 |
CHEMBL201013
pIC50 7.10
CHEMBL489
pIC50 7.89
CHEMBL1402
pIC50 7.89
CHEMBL418971
pKd 8.26
CHEMBL203472
pIC50 8.30
MDSVELCLPESFSLHYEEELLCRMSNKDRHIDSSCSSFIKTEPSSPASLTDSVNHHSPGGSSDASGSYSS 1 - 70 TMNGHQNGLDSPPLYPSAPILGGSGPVRKLYDDCSSTIVEDPQTKCEYMLNSMPKRLCLVCGDIASGYHY 71 - 140 GVASCEACKAFFKRTIQGNIEYSCPATNECEITKRRRKSCQACRFMKCLKVGMLKEGVRLDRVRGGRQKY 141 - 210 KRRIDAENSPYLNPQLVQPAKKPYNKIVSHLLVAEPEKIYAMPDPTVPDSDIKALTTLCDLADRELVVII 211 - 280 GWAKHIPGFSTLSLADQMSLLQSAWMEILILGVVYRSLSFEDELVYADDYIMDEDQSKLAGLLDLNNAIL 281 - 350 QLVKKYKSMKLEKEEFVTLKAIALANSDSMHIEDVEAVQKLQDVLHEALQDYEAGQHMEDPRRAGKMLMT 351 - 420 LPLLRQTSTKAVQHFYNIKLEGKVPMHKLFLEMLEAKV 421 - 458 //
