| Tclin | Delta-type opioid receptor |
Comments
Property Summary
| NCBI Gene PubMed Count | 107 |
| Grant Count | 22 |
| R01 Count | 10 |
| Funding | $2,679,592.84 |
| PubMed Score | 93.00 |
| PubTator Score | 83.55 |
| Disease | log2 FC | p |
|---|---|---|
| astrocytic glioma | -1.800 | 0.001 |
| ependymoma | -1.900 | 0.001 |
| oligodendroglioma | -1.700 | 0.001 |
| medulloblastoma | -2.200 | 0.000 |
| atypical teratoid / rhabdoid tumor | -2.000 | 0.000 |
| primitive neuroectodermal tumor | -1.900 | 0.004 |
| pilocytic astrocytoma | -1.300 | 0.002 |
eluxadoline
pKi 8.89
nalbuphine
pKi 6.00
naltrexone
pKi 7.99
oxymorphone
pKi 7.30
nalmefene
pKd 9.04
naloxone
pKi 7.12
morphine
pKi 7.24
hydromorphone
pKi 7.42
alvimopan
pKi 7.92
butorphanol
pKi 7.92
tramadol
pKi 8.03
buprenorphine
pKi 8.22
levorphanol
pIC50 8.29
CHEMBL3426794
pEC50 7.00
CHEMBL3426796
pEC50 7.00
CHEMBL3426792
pEC50 7.00
CHEMBL126918
pIC50 7.00
CHEMBL3808415
pKi 7.00
CHEMBL3350127
pKi 7.00
CHEMBL353938
pKi 7.00
CHEMBL258294
pKi 7.00
CHEMBL1161430
pKi 7.00
CHEMBL2048763
pKi 7.00
CHEMBL199294
pKi 7.00
CHEMBL355202
pKi 7.00
CHEMBL1076577
pKi 7.00
CHEMBL409036
pKi 7.00
CHEMBL117183
pKi 7.01
CHEMBL340724
pIC50 7.01
CHEMBL3667195
pKi 7.01
CHEMBL353303
pKi 7.01
CHEMBL201453
pKi 7.01
CHEMBL1907787
pKi 7.02
| AID | Type | Active / Inconclusive / Inactive | Description |
|---|---|---|---|
| 1788 | other |
0 / 0 / 0 | Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Ancillary Activity |
| 1921 | other |
2 / 0 / 0 | Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator: Ancillary Activity |
| 2343 | confirmatory |
1 / 0 / 131 | HTS Image-Based Screen for Agonists of the DOR Receptor |
| 2356 | confirmatory |
3 / 0 / 129 | HTS Image-Based Screen for Antagonists of the DOR Receptor |
| 2357 | confirmatory |
1 / 0 / 61 | SAR Analysis of Antagonists of the DOR Receptor using an Image-Based Assay |
| 2370 | confirmatory |
1 / 0 / 61 | SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay |
| 2493 | confirmatory |
0 / 0 / 16 | SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay - Set 2 |
| 2498 | confirmatory |
0 / 0 / 20 | SAR Analysis of Antagonists of the DOR Receptor using an Image-Based Assay - Set 2 |
| 434974 | screening |
0 / 0 / 0 | Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen |
| 488824 | confirmatory |
0 / 0 / 34 | SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay - Set 3 |
| More... |
| PMID | Text |
|---|---|
| 26549838 | the expression of DOR was upregulated in the drugresistant human hepatocellular carcinoma cells. |
| 26402014 | Results suggest deltaOR-Phe27Cys variation modulates beta- and gamma-secretase activity in late-stage Alzheimer's disease likely via post-translational mechanisms |
| 26233486 | findings suggest that SNPs in opioid receptors and the PNOC genes are associated with NAS severity. |
| 26211551 | OPRD-mediated activation of ERK1/2 is via ligand-specific transactivation of EGFR. |
| 25439010 | We have established a delta opioid receptor-PKC-Nrf2 axis as a part of the mechanism underlying cytoprotection against hypoxia/reoxygenation injury |
| 25178105 | Analysis of the transcription factor POU2F3 revealed a DOPr-mediated extracellular signal-regulated kinase (ERK)-dependent downregulation of this factorThe delta-opioid receptor affects epidermal homeostasis |
| 24798333 | Taken together, the hdeltaOR appears to rely primarily on the CNX-mediated N-glycan-dependent QC that has the capacity to assist in folding |
| 24628261 | Activation of the delta opioid receptor promotes cutaneous wound healing by affecting keratinocyte intercellular adhesion and migration |
| 24413399 | crystal structure of the human delta-opioid receptor (delta-OR), revealing the presence and fundamental role of a sodium ion in mediating allosteric control of receptor functional selectivity and constitutive activity |
| 24126707 | findings suggest that rs581111 and rs52920 may be useful when considering treatment options for female opioid addicts, however, confirmation in an independent sample is warranted |
| More... |
MEPAPSAGAELQPPLFANASDAYPSACPSAGANASGPPGARSASSLALAIAITALYSAVCAVGLLGNVLV 1 - 70 MFGIVRYTKMKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELLCKAVLSIDYYNMFTSIFTLT 71 - 140 MMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVGVPIMVMAVTRPRDGAVVCMLQFPSPSWYWD 141 - 210 TVTKICVFLFAFVVPILIITVCYGLMLLRLRSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIF 211 - 280 VIVWTLVDIDRRDPLVVAALHLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRKPCGRPDPSSFSRARE 281 - 350 ATARERVTACTPSDGPGGGAAA 351 - 372 //
| PMID | Year | Title |
|---|---|---|
| 26549838 | 2016 | Downregulation of ? opioid receptor by RNA interference enhances the sensitivity of BEL/FU drug?resistant human hepatocellular carcinoma cells to 5?FU. |
| 26402014 | 2015 | Genetic Variation in ?-Opioid Receptor Associates with Increased ?- and ?-Secretase Activity in the Late Stages of Alzheimer's Disease. |
| 26233486 | 2015 | Variations in opioid receptor genes in neonatal abstinence syndrome. |
| 26211551 | 2015 | Role for engagement of ?-arrestin2 by the transactivated EGFR in agonist-specific regulation of ? receptor activation of ERK1/2. |
| 25439010 | 2015 | A novel mechanism for cytoprotection against hypoxic injury: ?-opioid receptor-mediated increase in Nrf2 translocation. |
| 25178105 | 2015 | The ?-opioid receptor affects epidermal homeostasis via ERK-dependent inhibition of transcription factor POU2F3. |
| 24798333 | 2014 | N-Glycan-dependent and -independent quality control of human ? opioid receptor N-terminal variants. |
| 24628261 | 2015 | Activation of the ?-opioid receptor promotes cutaneous wound healing by affecting keratinocyte intercellular adhesion and migration. |
| 24613828 | 2014 | ?-Opioid receptor activation reduces ?-synuclein overexpression and oligomer formation induced by MPP(+) and/or hypoxia. |
| 24413399 | 2014 | Molecular control of ?-opioid receptor signalling. |
| More... |
