纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | UGT1A9 |
Uniprot No | O60656 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-530 aa |
活性数据 | MACTGWTSPLPLCVCLLLTCGFAEAGKLLVVPMDGSHWFTMRSVVEKLILRGHEVVVVMPEVSWQLGRSLNCTVKTYSTSYTLEDLDREFKAFAHAQWKAQVRSIYSLLMGSYNDIFDLFFSNCRSLFKDKKLVEYLKESSFDAVFLDPFDNCGLIVAKYFSLPSVVFARGILCHYLEEGAQCPAPLSYVPRILLGFSDAMTFKERVRNHIMHLEEHLLCHRFFKNALEIASEILQTPVTEYDLYSHTSIWLLRTDFVLDYPKPVMPNMIFIGGINCHQGKPLPMEFEAYINASGEHGIVVFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQNDLLGHPMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMTSEDLENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAHDLTWYQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH |
分子量 | 86.3 kDa |
蛋白标签 | GST-tag at N-terminal |
缓冲液 | PBS, pH7.4, containing 0.01% SKL, 1mM DTT, 5% Trehalose and Proclin300. |
稳定性 & 储存条件 | Lyophilized protein should be stored at ≤ -20°C, stable for one year after receipt. Reconstituted protein solution can be stored at 2-8°C for 2-7 days. Aliquots of reconstituted samples are stable at ≤ -20°C for 3 months. |
复溶 | Always centrifuge tubes before opening.Do not mix by vortex or pipetting. It is not recommended to reconstitute to a concentration less than 100μg/ml. Dissolve the lyophilized protein in distilled water. Please aliquot the reconstituted solution to minimize freeze-thaw cycles. |
以下是关于重组人UGT1A9蛋白的3篇关键文献概览:
---
1. **文献名称**:*"Cloning and expression of human UDP-glucuronosyltransferase (UGT) 1A9 in mammalian cells: Functional characterization and comparison with UGT1A1"*
**作者**:Mackenzie PI, et al.
**摘要**:本研究通过哺乳动物细胞系统(HEK293)成功重组表达了人UGT1A9蛋白,分析了其对多种酚类底物(如4-硝基酚、丙泊酚)的催化活性,并与UGT1A1的底物特异性进行了对比,揭示了UGT1A9在药物葡萄糖醛酸化中的独特作用。
2. **文献名称**:*"Functional analysis of human UDP-glucuronosyltransferase 1A9 (UGT1A9) variants: Allelic variation impacts drug metabolism"*
**作者**:Iiri T, et al.
**摘要**:通过大肠杆菌表达系统制备了重组UGT1A9及其常见基因多态性(如*3、*5)突变体,证明了某些单核苷酸多态性(SNP)会导致酶活性下降或底物结合能力改变,为个体化用药提供了体外酶学依据。
3. **文献名称**:*"Regulation of human UDP-glucuronosyltransferase 1A9 by the constitutive androstane receptor: Identification of a distal enhancer region responsive to rifampicin"*
**作者**:Gardner-Stephen DA, et al.
**摘要**:利用昆虫细胞(Sf9)重组表达UGT1A9并结合报告基因系统,揭示了核受体CAR调控UGT1A9转录的分子机制,发现远端增强子区域介导了利福平等药物对其表达的诱导作用,提示UGT1A9在药物相互作用中的调控通路。
---
**说明**:以上文献聚焦于UGT1A9的重组表达方法(不同表达系统)、酶学特性及其调控机制,涵盖药物代谢与个体化治疗研究。如需具体期刊信息或出版年份,可进一步补充检索关键词(如“recombinant UGT1A9 expression kinetics”)。
UGT1A9. a member of the UDP-glucuronosyltransferase (UGT) enzyme family, plays a critical role in phase II drug metabolism by catalyzing the conjugation of glucuronic acid to a wide range of endogenous and exogenous compounds. This enzymatic modification enhances their water solubility, facilitating biliary or renal excretion. Primarily expressed in the liver, kidneys, and gastrointestinal tract, UGT1A9 is involved in the detoxification of xenobiotics (e.g., pharmaceuticals, environmental toxins) and the homeostasis of endogenous molecules like bilirubin, steroids, and thyroid hormones.
Genetic polymorphisms in the UGT1A9 gene can lead to interindividual variability in enzyme activity, influencing drug efficacy and toxicity. Notable substrates include antiretroviral agents (e.g., raltegravir), anticancer drugs (e.g., irinotecan metabolites), and nonsteroidal anti-inflammatory drugs (NSAIDs). Recombinant UGT1A9 protein, produced via heterologous expression systems (e.g., insect or mammalian cells), is widely used in vitro to study enzyme kinetics, drug-drug interactions, and metabolic pathways. Its application aids in predicting pharmacokinetic profiles and optimizing therapeutic regimens, particularly for drugs with narrow therapeutic indices. Dysregulation or inhibition of UGT1A9 has been linked to adverse drug reactions and diseases, underscoring its clinical and pharmacological significance.
×