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  4. Recombinant Human UDP-glucuronosyltransferase 1A9 (UGT1A9)

Recombinant Human UDP-glucuronosyltransferase 1A9 (UGT1A9)

  • 货号：
    CSB-CF025582HU
  • 规格：
  • 来源：
    in vitro E.coli expression system
  • 其他：

产品详情

  • 基因名：
    UGT1A9
  • Uniprot No.：
  • 别名：
    UGT1A9; GNT1; UGT1; UDP-glucuronosyltransferase 1A9; UGT1A9; UDP-glucuronosyltransferase 1-9; UDPGT 1-9; UGT1*9; UGT1-09; UGT1.9; UDP-glucuronosyltransferase 1-I; UGT-1I; UGT1I; lugP4
  • 种属：
    Homo sapiens (Human)
  • 蛋白长度：
    Full Length of Mature Protein
  • 表达区域：
    26-530
  • 氨基酸序列
    GKLLVVPMDGSHWFTMRSVVEKLILRGHEVVVVMPEVSWQLGRSLNCTVKTYSTSYTLEDLDREFKAFAHAQWKAQVRSIYSLLMGSYNDIFDLFFSNCRSLFKDKKLVEYLKESSFDAVFLDPFDNCGLIVAKYFSLPSVVFARGILCHYLEEGAQCPAPLSYVPRILLGFSDAMTFKERVRNHIMHLEEHLLCHRFFKNALEIASEILQTPVTEYDLYSHTSIWLLRTDFVLDYPKPVMPNMIFIGGINCHQGKPLPMEFEAYINASGEHGIVVFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQNDLLGHPMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMTSEDLENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAHDLTWYQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
    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：
    UDP-glucuronosyltransferase (UGT) that catalyzes phase II biotransformation reactions in which lipophilic substrates are conjugated with glucuronic acid to increase the metabolite's water solubility, thereby facilitating excretion into either the urine or bile. Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds. Catalyzes the glucuronidation of endogenous estrogen hormones such as estradiol and estrone. Also catalyzes the glucuronidation of the isoflavones genistein, daidzein, glycitein, formononetin, biochanin A and prunetin, which are phytoestrogens with anticancer and cardiovascular properties. Involved in the glucuronidation of the AGTR1 angiotensin receptor antagonist caderastan, a drug which can inhibit the effect of angiotensin II. Involved in the biotransformation of 7-ethyl-10-hydroxycamptothecin (SN-38), the pharmacologically active metabolite of the anticancer drug irinotecan. Also metabolizes mycophenolate, an immunosuppressive agent.; Lacks UGT glucuronidation activity but acts as a negative regulator of isoform 1.
  • 基因功能参考文献：
    1. Icaritin was subjected to significant glucuronidation, wherein UGT1A3, 1A7, 1A8, 1A9 and 2B7 were main contributing enzymes. PMID: 28443723
    2. Inter-isoform Hetero-dimerization of Human UDP-Glucuronosyltransferases (UGTs) 1A1, 1A9, and 2B7 and Impacts on Glucuronidation Activity PMID: 27857056
    3. The findings of the study highlighted correlation between UGT1A9 -440C/T gene polymorphisms and positive propofol efficacy in patients undergoing painless induced pregnancy termination procedures. PMID: 28899924
    4. A significantly higher number of UGT1A9 polymorphisms was found in the group that did not respond to Mycophenolic acid treatment. PMID: 27549213
    5. None of the patients with Regorafenib-induced severe toxic hepatitis had CYP3A4 gene mutations. Similar polymorphisms in UGT1A9 gene promoter region were found in both patients who presented acute hepatitis. PMID: 27500989
    6. No association between the UGT1A9 c.98T>C polymorphism and mycophenolic acid plasma levels were found in renal transplant patients. PMID: 28613375
    7. UGT1A1, UGT1A6, and UGT1A9 were the chief contributors to the regioselective glucuronidation of diosmetin and chrysoeriol in the liver. PMID: 27832172
    8. polymorphisms c.98T>C in the UGT1A9 and c.1075A>C in the CYP2C9 genes did not affect the pharmacokinetic profile of propofol PMID: 27826892
    9. Carriers of T-275A and C-2152T single-nucleotide polymorphisms of the UGT1A9 gene promoter region show a greater incidence of death from digestive system cancer after kidney transplantation. PMID: 27932114
    10. demonstrated the effects of UGT1A9 genetic polymorphisms on MHD plasma concentrations and OXC therapeutic efficacy. Through MHD monitoring, we can predict OXC therapeutic efficacy, which may be useful for the personalization of OXC therapy in epileptic patients PMID: 27900402
    11. Dimerization changed the chemical regioselectivity, substrate-binding affinity, and enzymatic activity of UGT1A1 and UGT1A9 in glucuronidation of quercetin. PMID: 27025983
    12. UGT1A9 contributes to the in-vitro glucuronidation of arctigenin in liver microsomes. PMID: 26407805
    13. Suggest that the enzymatic properties of UGT1A9 are considerably different between humans and cynomolgus monkeys, although humUGT1A9 and monUGT1A9 were highly conserved at the amino acid level. PMID: 24470170
    14. We observed statistically significant associations between SNP and Drug-induced liver injury at both allele and genotype levels of of UGT1A9 promoter PMID: 25446781
    15. in tumor liver microsomes from HCC patients, either V(max) (maximum reaction rate, R(max) for UGT1A1) or clearance rates (V(max)/K(m), Clint) of UGT1A, UGT1A1, UGT1A4, UGT1A9 and UGT2B7 were lower than those in the adjacent normal liver microsomes PMID: 26010150
    16. Significantly lower estimated glomerular filtration rate of the renal allograft in UGT1A9 c.98C carriers did not translate into decreased allograft survival. PMID: 25380893
    17. Data shows that UGT1A9*22 allele was significantly less frequent in the Uzbek population compared to the Japanese. PMID: 24453052
    18. UGT1A9 is the major isoform responsible for the glucuronidations of fraxetin in liver microsomes. PMID: 24025985
    19. In HeLa cells overexpressing UGT1A9 there was an increase in catalysis and production of luteolin glucuronides. PMID: 24092055
    20. the UGT1A9 proximal promoter was assumed to change into the non-active form from the original sequence, and this might be one of the reasons for the tissue-specific expression of UGT1A9. PMID: 23842475
    21. UGT1A9 is a major contributor for (R) and (S) glucuronidation in the human liver and kidney. PMID: 23527766
    22. Alleles UGT1A9*4 and UGT1A9*5 were not present in any of the subjects of Polish population. PMID: 23184343
    23. determined the kinetics of efflux of 13 flavonoid glucuronides using the newly developed HeLa-UGT1A9 cells and correlated them with kinetic parameters derived using expressed UGT1A9 PMID: 23402418
    24. Data suggest that the substrate specificity of UGT1A9 includes the antiviral drug arbidol; UGT1A9 appears to be the major UGT isoform involved in the formation of arbidol glucuronides by liver microsomes. PMID: 23488780
    25. UGT1A9 and 2B7 are the main enzymes involved in ethanol glucuronidation. In addition, our results suggest that cannabinol and cannabidiol could significantly alter ethanol glucuronidation. PMID: 23230132
    26. none of the SNPs in UGT1A9 were present in our study population PMID: 23700788
    27. genetic association studies in pediatric population in United States: Data suggest that combined SNPs in UGT1A9, UGT2B7, and MRP2 are important in pharmacokinetics/biotransformation of prodrug mycophenolate mofetil in kidney transplant recipients. PMID: 23131697
    28. In Parkinson's disease patients UDP-glucuronosyltransferase 1A9 genotypes are associated with adverse reactions to to catechol-O-methyltransferase inhibitors PMID: 22527346
    29. increased cumulated drug exposure and UGT1A9 polymorphism (rs17868320) identified patients at high risk for early sorafenib-induced severe toxicity PMID: 22912756
    30. Expression of UGT1A9 correlated with age only in children younger than 1 year (Spearman r = 0.70). PMID: 22492655
    31. Study indicates that genotype status of UGT1A1, UGT1A9, and ABCC2 and serum bilirubin concentration increases reflect abnormally high AUC in patients treated with sorafenib. PMID: 22307138
    32. Report molecular models that can predict phenol substrate selectivity and in vitro clearance of UGT1A9. PMID: 22302521
    33. Investigation of morinidazole glucuronidation using human liver microsomes (HLMs) and 12 recombinant UDP glucuronosyltransferases (UGTs) indicated that this biotransformation was mainly catalyzed by UGT1A9. PMID: 22184458
    34. Data suggest that darexaban glucuronidation in liver microsomes is mainly catalyzed by UGT1A9; studies include kinetics of recombinant UGT proteins, liver microsomes, and jejunal microsomes (and UGT isoform-specific inhibitors/substrates). PMID: 22031623
    35. transplanted kidney function may be affected in patients carrying UGT1A9 98C allele and receiving mycophenolate mophetil PMID: 22210424
    36. The presence of BSA during the glucuronidation reaction leads to a large increase in the V(max) value of UGT1A9, in addition to lowering its K(m) value. PMID: 21856742
    37. A significantly stereoselective difference on the glucuronidation of rac-FPF was seen between the two variants compared with the wild type of UGT1A9. PMID: 21856293
    38. In a study of Japanese renal transplant recipients, there are no significant differences in the area under the plasma concentration-time curve ratio of mycophenolic acid glucuronide/MPA between UGT1A9 I399C/T genotypes. PMID: 18695635
    39. analysis of stereoselective metabolism of propranolol glucuronidation by human UDP-glucuronosyltransferases 2B7 and 1A9 PMID: 19644937
    40. Further mutagenesis and activity assays suggested that Phe117 of UGT1A9 participates in 1-naphthol binding PMID: 20089735
    41. Data point to UGT1A9 as main UGT isoform in liver microsomes metabolizing psilocin (a hallucinogenic indole alkaloid); kinetic studies are included. PMID: 20007669
    42. N-glycosylation has an important role in the folding of UGT1A9. PMID: 19951703
    43. In this study, we sequenced the promoter and exon 1 regions of the UGT1A9 gene in 93 Thai individuals and identified 7 genetic polymorphisms PMID: 19881262
    44. Carriers of single nucleotide polymorphisms in this protein's promotor region show a greater incidence of gastrointestinal side effects and lower exposure to mycophenolic acid. PMID: 19715905
    45. sequence of the cDNA segment cloned, 1666 bp in length. The recombinant constructed, pREP9-UGT1A9, contains the entire coding region, along with 18 bp of the 5' and 55 bp of the 3' untranslated region of theUGT1A9 cDNA. PMID: 11854913
    46. 1A9 enzyme is a peroxisome proliferator-activated receptor alpha and gamma target gene PMID: 12582161
    47. a significant role for UGT1A9 and 2B7 in the catalysis of almokalant glucuronidation PMID: 14660172
    48. mutant allele with one base insertion in the promoter region of the UGT1A9 gene would alter the level of enzyme expression and the metabolism of those drugs that are substrates of UGT1A9 PMID: 15115919
    49. Study provides preliminary evidence that genetic factors, especially in hepatic UGT1A9, may contribute to the variability of mycophenolic acid pharmacokinetics observed in transplant patients. PMID: 15258099
    50. stereoselectivity for etodolac PMID: 15370961

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  • 亚细胞定位：
    Endoplasmic reticulum membrane; Single-pass membrane protein.
  • 蛋白家族：
    UDP-glycosyltransferase family
  • 组织特异性：
    [Isoform 1]: Expressed in liver, kidney, colon, esophagus and small intestine.; [Isoform 2]: Expressed in liver, kidney, colon, esophagus and small intestine.
  • 数据库链接：

    HGNC: 12541

    OMIM: 191740

    KEGG: hsa:54600

    STRING: 9606.ENSP00000346768

    UniGene: Hs.554822