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  5. Delta-type opioid receptor

Tclin Delta-type opioid receptor

G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain and in opiate-mediated analgesia. Plays a role in developing analgesic tolerance to morphine.

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Property Summary

NCBI Gene PubMed Count 107
PubMed Score 93.00
PubTator Score 83.55

Knowledge Summary

Patent (2,943)

TINX Plot

  Disease Sources (4)

Disease Target Count P-value
atypical teratoid / rhabdoid tumor 4369 2.42413572894913E-6
medulloblastoma 1524 5.02956455013294E-6
ependymoma 2514 9.991391219439E-4
astrocytic glioma 2241 0.0011394454707284
oligodendroglioma 2849 0.00140290966302561
pilocytic astrocytoma 3086 0.00172355740161383
primitive neuroectodermal tumor 3031 0.00415902986389957

Expression

  Differential Expression (7)

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

Synonym

Accession P41143 B5B0B8 D-OR-1
Symbols OPRD

Gene

OPRD1

PANTHER Protein Class (2)

PDB

1OZC   2IQM   4N6H   4RWA   4RWD  

  Ortholog (9)

Species Source
Chimp OMA EggNOG
Macaque OMA EggNOG Inparanoid
Mouse OMA EggNOG Inparanoid
Rat OMA EggNOG Inparanoid
Dog OMA EggNOG Inparanoid
Cow OMA EggNOG
Opossum OMA EggNOG Inparanoid
Anole lizard OMA Inparanoid
Xenopus OMA EggNOG

  TechDev Info (1)

Bryan Roth functional assay

 GO Function (3)

 GO Component (10)

 GO Process (22)

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 Compartment GO Term (21)

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 MGI Term (4)

 GWAS Trait (1)

 HCA RNA Cell Line (56)

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Pathway (23)

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 UniProt Keyword (16)

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Drug (13)  

Structure of eluxadoline

eluxadoline
pKi 8.89

Structure of nalbuphine

nalbuphine
pKi 6.00

Structure of naltrexone

naltrexone
pKi 7.99

Structure of oxymorphone

oxymorphone
pKi 7.30

Structure of nalmefene

nalmefene
pKd 9.04

Structure of naloxone

naloxone
pKi 7.12

Structure of morphine

morphine
pKi 7.24

Structure of hydromorphone

hydromorphone
pKi 7.42

Structure of alvimopan

alvimopan
pKi 7.92

Structure of butorphanol

butorphanol
pKi 7.92

Structure of tramadol

tramadol
pKi 8.03

Structure of buprenorphine

buprenorphine
pKi 8.22

Structure of levorphanol

levorphanol
pIC50 8.29

Ligand (1,548)  

Structure of CHEMBL3426794

CHEMBL3426794
pEC50 7.00

Structure of CHEMBL3426796

CHEMBL3426796
pEC50 7.00

Structure of CHEMBL3426792

CHEMBL3426792
pEC50 7.00

Structure of CHEMBL126918

CHEMBL126918
pIC50 7.00

Structure of CHEMBL3808415

CHEMBL3808415
pKi 7.00

Structure of CHEMBL3350127

CHEMBL3350127
pKi 7.00

Structure of CHEMBL353938

CHEMBL353938
pKi 7.00

Structure of CHEMBL258294

CHEMBL258294
pKi 7.00

Structure of CHEMBL1161430

CHEMBL1161430
pKi 7.00

Structure of CHEMBL2048763

CHEMBL2048763
pKi 7.00

Structure of CHEMBL199294

CHEMBL199294
pKi 7.00

Structure of CHEMBL355202

CHEMBL355202
pKi 7.00

Structure of CHEMBL1076577

CHEMBL1076577
pKi 7.00

Structure of CHEMBL409036

CHEMBL409036
pKi 7.00

Structure of CHEMBL117183

CHEMBL117183
pKi 7.01

Structure of CHEMBL340724

CHEMBL340724
pIC50 7.01

Structure of CHEMBL3667195

CHEMBL3667195
pKi 7.01

Structure of CHEMBL353303

CHEMBL353303
pKi 7.01

Structure of CHEMBL201453

CHEMBL201453
pKi 7.01

Structure of CHEMBL1907787

CHEMBL1907787
pKi 7.02

MLP Assay (40)

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
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Gene RIF (83)

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
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AA Sequence 

MEPAPSAGAELQPPLFANASDAYPSACPSAGANASGPPGARSASSLALAIAITALYSAVCAVGLLGNVLV      1 - 70
MFGIVRYTKMKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELLCKAVLSIDYYNMFTSIFTLT     71 - 140
MMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVGVPIMVMAVTRPRDGAVVCMLQFPSPSWYWD    141 - 210
TVTKICVFLFAFVVPILIITVCYGLMLLRLRSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIF    211 - 280
VIVWTLVDIDRRDPLVVAALHLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRKPCGRPDPSSFSRARE    281 - 350
ATARERVTACTPSDGPGGGAAA                                                    351 - 372
//

Text Mined References (108)

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.
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