| Tclin | Thyroid hormone receptor alpha |
The protein encoded by this gene is a nuclear hormone receptor for triiodothyronine. It is one of the several receptors for thyroid hormone, and has been shown to mediate the biological activities of thyroid hormone. Knockout studies in mice suggest that the different receptors, while having certain extent of redundancy, may mediate different functions of thyroid hormone. Alternatively spliced transcript variants encoding distinct isoforms have been reported. [provided by RefSeq, Jul 2008]
Comments
Property Summary
| NCBI Gene PubMed Count | 132 |
| Grant Count | 80 |
| R01 Count | 32 |
| Funding | $11,287,527.85 |
| PubMed Score | 522.91 |
| PubTator Score | 229.05 |
| Disease | log2 FC | p |
|---|---|---|
| malignant mesothelioma | -1.400 | 0.000 |
| psoriasis | -2.100 | 0.000 |
| osteosarcoma | -2.119 | 0.000 |
| glioblastoma | -1.600 | 0.010 |
| atypical teratoid / rhabdoid tumor | -1.900 | 0.000 |
| medulloblastoma, large-cell | -1.400 | 0.000 |
| breast carcinoma | -1.500 | 0.000 |
| pediatric high grade glioma | -1.300 | 0.009 |
| sonic hedgehog group medulloblastoma | -1.200 | 0.000 |
| subependymal giant cell astrocytoma | -1.276 | 0.009 |
| lung adenocarcinoma | -1.600 | 0.000 |
| ovarian cancer | -1.200 | 0.000 |
CHEMBL3126376
pEC50 7.00
CHEMBL250104
pIC50 7.00
CHEMBL236438
pIC50 7.00
CHEMBL195079
pIC50 7.00
CHEMBL392925
pIC50 7.02
CHEMBL109279
pKd 7.03
CHEMBL238178
pIC50 7.03
CHEMBL2312262
pKi 7.04
CHEMBL3397346
pKi 7.05
CHEMBL236499
pIC50 7.06
CHEMBL264153
pEC50 7.06
CHEMBL249445
pIC50 7.07
CHEMBL440975
pIC50 7.08
CHEMBL264410
pKd 7.09
CHEMBL250308
pIC50 7.11
CHEMBL2035879
pKi 7.16
CHEMBL485928
pKi 7.21
CHEMBL372428
pIC50 7.21
CHEMBL235384
pIC50 7.30
CHEMBL193615
pIC50 7.32
| AID | Type | Active / Inconclusive / Inactive | Description |
|---|---|---|---|
| 2277 | screening |
14 / 0 / 0 | Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. |
| 504934 | other |
1 / 0 / 0 | Late stage assay provider results from the probe development effort to identify inverse agonists of the liver receptor homolog-1 (LRH-1; NR5A2): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors |
| PMID | Text |
|---|---|
| 26585273 | 8 different THRA gene abnormalities have been described in 14 patients from 9 families with phenotypes including short stature, dysmorphic syndrome, psychoneuromotor disorders, constipation and bradycardia. Review. |
| 26029931 | The current study aimed to investigate whether TRs may be specifically expressed in BRCA1 associated cancer cases. |
| 25670821 | THRA mutations may be more common than expected. In patients with clinical symptoms of mild hypothyreosis without confirmation in endocrine studies, a molecular study of THRA defects is strongly recommended. |
| 25542270 | Thyroid hormone signalling may be important in a proportion of breast cancers and THRalpha2 expression may be a regulator of signalling in this pathway. |
| 25501869 | Thyroid hormone receptor (TRalpha1) is shown to occur and determine postischemic remodeling and cardiac recovery depending on the availability of TH. [review] |
| 25079464 | THRalpha rs939348 polymorphism was associated with L-T4 dose and central obesity among hypothyroid patients. |
| 24969835 | Data suggest thyroid hormone resistance syndrome can be exhibited by patients with heterozygous missense mutation (Ala263Val) in THRA1 and THRA2, isoforms resulting from alternative splicing. [CASE REPORT] |
| 24914936 | Thyroid hormone receptor alpha mutation is associated with a severe and thyroxine-resistant skeletal dysplasia. |
| 24673558 | Transactivation of reporter genes in response to T4 thyroid hormone was dependent on the thyroid hormone receptor subtypes in human cells. |
| 24552590 | A new x-ray crystallographic structure of thyroid hormone receptor ligand-binding domains shows a second binding site for thyroid hormones. |
| More... |
MEQKPSKVECGSDPEENSARSPDGKRKRKNGQCSLKTSMSGYIPSYLDKDEQCVVCGDKATGYHYRCITC 1 - 70 EGCKGFFRRTIQKNLHPTYSCKYDSCCVIDKITRNQCQLCRFKKCIAVGMAMDLVLDDSKRVAKRKLIEQ 71 - 140 NRERRRKEEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNAQGSHWKQRRKFLPDDIGQSPIVSMPDGDKV 141 - 210 DLEAFSEFTKIITPAITRVVDFAKKLPMFSELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEM 211 - 280 AVKREQLKNGGLGVVSDAIFELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFE 281 - 350 HYVNHRKHNIPHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQGPQVRQLEQQL 351 - 420 GEAGSLQGPVLQHQSPKSPQQRLLELLHRSGILHARAVCGEDDSSEADSPSSSEEEPEVCEDLAGNAASP 421 - 490 //
| PMID | Year | Title |
|---|---|---|
| 26585273 | 2015 | TR? receptor mutations extend the spectrum of syndromes of reduced sensitivity to thyroid hormone. |
| 26037512 | 2015 | A Novel Mutation in THRA Gene Associated With an Atypical Phenotype of Resistance to Thyroid Hormone. |
| 26029931 | 2015 | Thyroid Hormone Receptors Predict Prognosis in BRCA1 Associated Breast Cancer in Opposing Ways. |
| 25670821 | 2015 | Thyroid hormone resistance syndrome due to mutations in the thyroid hormone receptor ? gene (THRA). |
| 25542270 | 2015 | Thyroid hormone receptor ? in breast cancer: prognostic and therapeutic implications. |
| 25501869 | 2015 | Translating thyroid hormone effects into clinical practice: the relevance of thyroid hormone receptor ?1 in cardiac repair. |
| 25416956 | 2014 | A proteome-scale map of the human interactome network. |
| 25079464 | The associations of polymorphisms of TSH receptor and thyroid hormone receptor genes with L-thyroxine treatment in hypothyroid patients. | |
| 24969835 | 2014 | Resistance to thyroid hormone caused by a mutation in thyroid hormone receptor (TR)?1 and TR?2: clinical, biochemical, and genetic analyses of three related patients. |
| 24914936 | 2014 | Thyroid hormone receptor ? mutation causes a severe and thyroxine-resistant skeletal dysplasia in female mice. |
| More... |
