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  4. Recombinant Human Kappa-type opioid receptor (OPRK1)

Recombinant Human Kappa-type opioid receptor (OPRK1)

  • 货号：
    CSB-CF016359HU
  • 规格：
  • 来源：
    in vitro E.coli expression system
  • 其他：

产品详情

  • 基因名：
  • Uniprot No.：
  • 别名：
    OPRK1; OPRK; Kappa-type opioid receptor; K-OR-1; KOR-1
  • 种属：
    Homo sapiens (Human)
  • 蛋白长度：
    Full length protein
  • 表达区域：
    1-380
  • 氨基酸序列
    MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV RNTVQDPAYLRDIDGMNKPV
    Note: The complete sequence including tag sequence, target protein sequence and linker sequence could be provided upon request.
  • 蛋白标签：
    N-terminal 10xHis-tagged
  • 产品提供形式：
    Liquid or 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.
  • 缓冲液：
    Lyophilized from Tris/PBS-based buffer, 6% Trehalose, pH 8.0
  • 储存条件：
    Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. Avoid repeated freeze-thaw cycles.
  • 保质期：
    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.
  • 货期：
    Basically, we can dispatch the products out in 1-3 working days after receiving your orders. 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.
  • 注意事项：
    Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.
  • Datasheet & COA：
    Please contact us to get it.

产品评价

靶点详情

  • 功能：
    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.
  • 基因功能参考文献：
    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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  • 亚细胞定位：
    Cell membrane; Multi-pass membrane protein.
  • 蛋白家族：
    G-protein coupled receptor 1 family
  • 组织特异性：
    Detected in brain and placenta.
  • 数据库链接：

    HGNC: 8154

    OMIM: 165196

    KEGG: hsa:4986

    STRING: 9606.ENSP00000265572

    UniGene: Hs.106795