Recombinant Human Kappa-type opioid receptor (OPRK1)

Code CSB-CF016359HU
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Source in vitro E.coli expression system
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Product Details

Target Names
OPRK1
Uniprot No.
Alternative Names
OPRK1; OPRK; Kappa-type opioid receptor; K-OR-1; KOR-1
Species
Homo sapiens (Human)
Expression Region
1-380
Target Protein Sequence
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV RNTVQDPAYLRDIDGMNKPV
Protein Length
Full length protein
Tag Info
Tag type will be determined during the manufacturing process.
The tag type will be determined during production process. If you have specified tag type, please tell us and we will develop the specified tag preferentially.
Form
Lyophilized powder
Note: We will preferentially ship the format that we have in stock, however, if you have any special requirement for the format, please remark your requirement when placing the order, we will prepare according to your demand.
Buffer before Lyophilization
Tris/PBS-based buffer, 6% Trehalose, pH 8.0
Reconstitution
We recommend that this vial be briefly centrifuged prior to opening to bring the contents to the bottom. Please reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL.We recommend to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20℃/-80℃. Our default final concentration of glycerol is 50%. Customers could use it as reference.
Troubleshooting and FAQs
Storage Condition
Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. Avoid repeated freeze-thaw cycles.
Shelf Life
The shelf life is related to many factors, storage state, buffer ingredients, storage temperature and the stability of the protein itself.
Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.
Lead Time
Delivery time may differ from different purchasing way or location, please kindly consult your local distributors for specific delivery time.
Note: All of our proteins are default shipped with normal blue ice packs, if you request to ship with dry ice, please communicate with us in advance and extra fees will be charged.
Notes
Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.
Datasheet
Please contact us to get it.

Customer Reviews and Q&A

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Target Background

Function
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. 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. Plays a role in mediating reduced physical activity upon treatment with synthetic opioids. Plays a role in the regulation of salivation in response to synthetic opioids. May play a role in arousal and regulation of autonomic and neuroendocrine functions.
Gene References into Functions
  1. The OPRK1 gene variants showed significant association with susceptibility to opioid dependence among Iranians. PMID: 28786760
  2. Down-regulation of KOR in HCC tumour tissues has a strong association with poor prognosis and KOR might be a potential tumour suppressor. PMID: 28821282
  3. In HUVEC cells subjected to artificial hyperlipidemia, selective agonists and antagonists showed that kappa-opioid receptor stimulation normalizes endothelial ultrastructure and function under hyperlipidemic conditions via the PI3K/Akt/eNOS pathway. PMID: 27226238
  4. The OPRK1/kappa-opioid receptor pathway was found to be downregulated in lesional skin of psoriasis, correlating positively with itch sensation. PMID: 27958613
  5. These results indicate that KOR can form a heterodimer with B2R and this leads to increased protein kinase A activity by the CREB signaling pathway, leading to a significant increase in cell proliferation. PMID: 28069442
  6. that promoter fragments of OPRK1 and OPRM1 were able to upregulate gene expression with mild cognitive impairment PMID: 27838450
  7. Hypoxia inducible factor-1alpha (HIF-1alpha) siRNA knocked down the increase of endogenous HIF-1alpha messages and diminished the desferrioxamine (DFO)-induced increase of kappa-opioid receptor (hKOR) expression. PMID: 28117678
  8. genetic association studies in a population in Denmark: Data suggest that carriers/heterozygotes of the C allele (CC/CT) of OPRK SNP rs6473799 report a 30.4% higher mechanical visceral pain tolerance threshold than non-carriers. PMID: 27061127
  9. Molecular switches of the kappa opioid receptor triggered by 6'-GNTI and 5'-GNTI have been described. PMID: 26742690
  10. data provide evidence for genetic modulation of opioid withdrawal severity. PMID: 26692286
  11. OPRK1 promoter hypermethylation might increase the risk of AD through its regulation on the gene expression of OPRK1. PMID: 26300544
  12. OX1R and KOR heterodimerize, and this heterodimer associates with Galphas, leading to increased protein kinase A (PKA) signaling pathway activity, including upregulation of intracellular cAMP levels. PMID: 25866368
  13. The structure of the dynorphin (1-13) peptide (dynorphin) bound to the human kappa opioid receptor (KOR) has been determined by liquid-state NMR spectroscopy. PMID: 26372966
  14. RGS2 and RGS4 are new interacting partners that play key roles in G protein coupling to negatively regulate kappa-OmicronR signaling. PMID: 25289860
  15. Data show that the crystallographic structures of the mouse mu-opioid receptor (MOPr) and human kappa-opioid receptor (KOPr) indicate putative interfacial interactions. PMID: 24651466
  16. Here we describe three experimental procedures we used to evaluate the interaction between hKOPR and 14-3-3zeta: co-immunoprecipitation, pull-down assay and immunofluorescence microscopy. PMID: 25293321
  17. Studied differential DNA-protein interactions of PDYN and OPRK1 SNPs significantly associated with alcohol dependence. PMID: 25177835
  18. Results suggest that Kappa receptor availability in an amygdala-cingulate cortex-striatal circuit mediates the phenotypic expression of trauma-related loss (ie, dysphoria) symptoms. PMID: 25229257
  19. Low OPRK1 expression is associated with liver metastases of small bowel neuroendocrine tumors. PMID: 25241033
  20. Data indicate that replacement of the 3-hydroxyl substituent of the 4-(3-hydroxyphenyl) group of JDTic with a H, F, or Cl substituent leads to potent and selective kappa opioid receptor (KOR) antagonists. PMID: 25133923
  21. findings suggest that genetic polymorphisms in OPRK1 were associated with the body weight, alcohol use, and opioid withdrawal symptoms in MMT patients. PMID: 24525640
  22. Suggest that methamphetamine induced early autophagic response is a survival mechanism for apoptotic endothelial cells and is mediated through the kappa opioid receptor. PMID: 24603327
  23. In heroin-dependent patients, no difference was evidenced between responders and non-reponders to buprenorphine therapy in the frequency of OPRK1 SNP. PMID: 24274990
  24. Neurocognitive and neuroinflammatory correlates of OPRK1 mRNA expression in the anterior cingulate in postmortem brain of HIV-infected subjects. PMID: 24405578
  25. This study indicates that a patient's OPRK1 genotype could be used to identify a subset of individuals for whom vaccine treatment may be an effective pharmacotherapy for cocaine dependence. PMID: 23995774
  26. OPRK1 rs6989250 C>G is associated with stress-induced craving and cortisol, hyperactive hypothalamus/thalamus-midbrain-cerebellum responses, and also associated with greater subsequent cocaine relapse risk. PMID: 23962922
  27. Data suggest that dynorphin A (DynA) is ligand for opioid receptor kappa (KOR); upon DynA binding, only small chemical shifts observed in second extracellular loop of KOR; chemical shift changes of DynA show conclusively that DynA interacts with KOR. PMID: 24616919
  28. crystal structure provides fundamental insights into the activation mechanism of the kappa-opioid receptor and suggest that "functional" residues may be directly involved in transduction of the agonist binding event PMID: 24121503
  29. Kappa Opioid receptor in the nucleus is a novel prognostic factor of esophageal squamous cell carcinoma. PMID: 23574786
  30. OPRK1 and PDYN polymorphisms may alter severity of HIV infection and response to treatment. PMID: 23392455
  31. Pairwise tag single nucleotide polymorphisms (SNPs) in DREAM, PDYN and OPRK1 were genotyped in a United Kingdom population-based discovery cohort in whom pain was assessed. PMID: 22730276
  32. hKOR activates p38 MAPK through a phosphorylation and arrestin-dependent mechanism; however, activation differs between hKOR and rKOR for some ligands PMID: 23086943
  33. Data indicate that 14-3-3zeta interaction with kappa-opioid receptor (hKOPR) C-tail promotes export of hKOPR. PMID: 22989890
  34. A role is estsablished for dynorphin kappa-opioid receptor signaling in fear extinction. PMID: 22764240
  35. crystal structure of the human kappa-OR in complex with the selective antagonist JDTic, arranged in parallel dimers, at 2.9 A resolution PMID: 22437504
  36. Human apelin forms a heterodimer with the kappa opioid receptor and leads to increased protein kinase C and decreased protein kinase A. PMID: 22200678
  37. In summary, this study provides evidence that gene-gene interaction between KOR and OPRM1 can influence the risk of addiction to narcotics and alcohol. PMID: 22138325
  38. These findings provide evidence that previously demonstrated KOR-mediated reduction in intraocular pressure could be caused, in part, by NO production in both the ciliary body and the trabecular meshwork. PMID: 21666232
  39. This is the first report detailing the initiation of a KOR-induced JAK2/STAT3 and IRF2 signaling cascade, and these pathways result in substantial down-regulation of CXCR4 expression. PMID: 21447649
  40. because of its stronger binding for hKOPR, GEC1 is able to be recruited by hKOPR sufficiently without membrane association via its C-terminal modification; however, du GABARAP appears to require C-terminal modifications to enhance KOPR expression. PMID: 21388957
  41. Review. kappa-Opioid receptor signaling and brain reward function. PMID: 19804796
  42. phosphorylation of serine 369 mediates KOR desensitization and internalization PMID: 12815037
  43. binding of the KOR to NHERF-1/EBP50 facilitates oligomerization of NHERF-1/EBP50, leading to stimulation of NHE3. PMID: 15070904
  44. OPKR1 structure and association of haplotypes with opiate addiction was found to have empirical significance. PMID: 15608558
  45. The diterpenoid salvinorin A utilizes unique residues within a commonly shared binding pocket to selectively activate KORs. PMID: 15952771
  46. GEC1 interacts with the kappa opioid receptor and enhances expression of the receptor PMID: 16431922
  47. Family-based analyses demonstrated associations between alcohol dependence and multiple SNPs in intron 2 of OPRK1. PMID: 16924269
  48. Helical orientation of helix 2 are critical for the selectivity of salvinorin A binding to KOR and provide a structurally novel basis for ligand selectivity. PMID: 17121830
  49. frequency of KOR 36G > T SNP was significantly higher among heroin-dependent individuals compared with control subjects PMID: 17373729
  50. activation of KORs alters functional properties of neural precursor cells that are relevant to human brain development and repair. PMID: 17538007

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Subcellular Location
Cell membrane; Multi-pass membrane protein.
Protein Families
G-protein coupled receptor 1 family
Tissue Specificity
Detected in brain and placenta.
Database Links

HGNC: 8154

OMIM: 165196

KEGG: hsa:4986

STRING: 9606.ENSP00000265572

UniGene: Hs.106795

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