| Tchem | Nuclear receptor subfamily 4 group A member 2 |
Transcriptional regulator which is important for the differentiation and maintenance of meso-diencephalic dopaminergic (mdDA) neurons during development. It is crucial for expression of a set of genes such as SLC6A3, SLC18A2, TH and DRD2 which are essential for development of mdDA neurons (By similarity).
This gene encodes a member of the steroid-thyroid hormone-retinoid receptor superfamily. The encoded protein may act as a transcription factor. Mutations in this gene have been associated with disorders related to dopaminergic dysfunction, including Parkinson disease, schizophernia, and manic depression. Misregulation of this gene may be associated with rheumatoid arthritis. Alternatively spliced transcript variants have been described, but their biological validity has not been determined. [provided by RefSeq, Jul 2008]
This gene encodes a member of the steroid-thyroid hormone-retinoid receptor superfamily. The encoded protein may act as a transcription factor. Mutations in this gene have been associated with disorders related to dopaminergic dysfunction, including Parkinson disease, schizophernia, and manic depression. Misregulation of this gene may be associated with rheumatoid arthritis. Alternatively spliced transcript variants have been described, but their biological validity has not been determined. [provided by RefSeq, Jul 2008]
Comments
Property Summary
| NCBI Gene PubMed Count | 147 |
| Grant Count | 160 |
| R01 Count | 92 |
| Funding | $11,886,893.36 |
| PubMed Score | 384.87 |
| PubTator Score | 263.74 |
CHEMBL246652
pEC50 7.11
CHEMBL246654
pEC50 7.23
CHEMBL393713
pEC50 7.50
CHEMBL247879
pEC50 7.59
CHEMBL399602
pEC50 8.39
CHEMBL401032
pEC50 8.41
CHEMBL399807
pEC50 8.46
CHEMBL399603
pEC50 9.10
| 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 |
|---|---|
| 26239742 | decreased expression levels of Nurr1 were associated with chronic inflammation and insulin resistance in patients with T2D. |
| 26148973 | Data show that some rexinoids display selective coactivator (CoA) recruitment by the retinoid X receptors (RXRs) homodimer and by the heterodimers nuclear receptor Nur77/RXR and Nurr1/RXR. |
| 26022133 | The immunohistochemical, qRT-PCR and western blot analyses revealed that Nurr1 expression was increased in gastric cancer tissues compared with normal gastric tissue. |
| 25982322 | The results failed to reveal significant link between NR4A2 polymorphism and schizophrenia risk. [META-ANALYSIS] |
| 25953901 | Thus our data identify a previously unknown role for Nr4a2 in the regulation of macrophage polarization. |
| 25917081 | NR4A2 is a key factor in multiple diseases, such as inflammation, cancer and cardiovascular diseases. |
| 25809189 | A2M is expressed in the vasculature and NR4A receptors modulate VSMC MMP2/9 activity by several mechanisms including the up-regulation of A2M. |
| 25752609 | Because the phosphorylation site mutants of NR4A2 cannot rescue the cell death-promoting activity, ASK1-p38 pathway-dependent phosphorylation and subsequent cytoplasmic translocation of NR4A2 may be required for oxidative stress-induced cell death. |
| 25503547 | NURR1 upregulation by tissue-type plasminogen activator during ischemic stroke is associated with endothelial dysfunction and inflammation. |
| 25199433 | gestational diabetes mellitus, but not pre-existing maternal obesity, associated with increased placental expression |
| More... |
MPCVQAQYGSSPQGASPASQSYSYHSSGEYSSDFLTPEFVKFSMDLTNTEITATTSLPSFSTFMDNYSTG 1 - 70 YDVKPPCLYQMPLSGQQSSIKVEDIQMHNYQQHSHLPPQSEEMMPHSGSVYYKPSSPPTPTTPGFQVQHS 71 - 140 PMWDDPGSLHNFHQNYVATTHMIEQRKTPVSRLSLFSFKQSPPGTPVSSCQMRFDGPLHVPMNPEPAGSH 141 - 210 HVVDGQTFAVPNPIRKPASMGFPGLQIGHASQLLDTQVPSPPSRGSPSNEGLCAVCGDNAACQHYGVRTC 211 - 280 EGCKGFFKRTVQKNAKYVCLANKNCPVDKRRRNRCQYCRFQKCLAVGMVKEVVRTDSLKGRRGRLPSKPK 281 - 350 SPQEPSPPSPPVSLISALVRAHVDSNPAMTSLDYSRFQANPDYQMSGDDTQHIQQFYDLLTGSMEIIRGW 351 - 420 AEKIPGFADLPKADQDLLFESAFLELFVLRLAYRSNPVEGKLIFCNGVVLHRLQCVRGFGEWIDSIVEFS 421 - 490 SNLQNMNIDISAFSCIAALAMVTERHGLKEPKRVEELQNKIVNCLKDHVTFNNGGLNRPNYLSKLLGKLP 491 - 560 ELRTLCTQGLQRIFYLKLEDLVPPPAIIDKLFLDTLPF 561 - 598 //
| PMID | Year | Title |
|---|---|---|
| 26871637 | 2016 | Widespread Expansion of Protein Interaction Capabilities by Alternative Splicing. |
| 26239742 | 2015 | Decreased expression levels of Nurr1 are associated with chronic inflammation in patients with type 2 diabetes. |
| 26148973 | 2015 | Selective ligand activity at Nur/retinoid X receptor complexes revealed by dimer-specific bioluminescence resonance energy transfer-based sensors. |
| 26022133 | 2015 | Clinicopathological significance of orphan nuclear receptor Nurr1 expression in gastric cancer. |
| 25982322 | 2015 | Association between NR4A2 genetic variation and schizophrenia: A comprehensive systematic review and meta-analysis. |
| 25953901 | 2015 | Nuclear Receptor Nr4a2 Promotes Alternative Polarization of Macrophages and Confers Protection in Sepsis. |
| 25917081 | 2016 | Nuclear receptor 4A (NR4A) family - orphans no more. |
| 25809189 | 2015 | NR4A receptors up-regulate the antiproteinase alpha-2 macroglobulin (A2M) and modulate MMP-2 and MMP-9 in vascular smooth muscle cells. |
| 25752609 | 2015 | Apoptosis Signal-regulating Kinase 1 (ASK1)-p38 Pathway-dependent Cytoplasmic Translocation of the Orphan Nuclear Receptor NR4A2 Is Required for Oxidative Stress-induced Necrosis. |
| 25503547 | 2015 | NURR1 involvement in recombinant tissue-type plasminogen activator treatment complications after ischemic stroke. |
| More... |
