纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | PIK4CA |
Uniprot No | P42356 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-854 aa |
活性数据 | MREMAGAWHMTVEQKFGLFSAEIKEADPLAASEASQPKPCPPEVTPHYIWIDFLVQRFEIAKYCSSDQVEIFSSLLQRSMSLNIGGAKGSMNRHVAAIGPRFKLLTLGLSLLHADVVPNATIRNVLREKIYSTAFDYFSCPPKFPTQGEKRLREDISIMIKFWTAMFSDKKYLTASQLVPPDNQDTRSNLDITVGSRQQATQGWINTYPLSSGMSTISKKSGMSKKTNRGSQLHKYYMKRRTLLLSLLATEIERLITWYNPLSAPELELDQAGENSVANWRSKYISLSEKQWKDNVNLAWSISPYLAVQLPARFKNTEAIGNEVTRLVRLDPGAVSDVPEAIKFLVTWHTIDADAPELSHVLCWAPTDPPTGLSYFSSMYPPHPLTAQYGVKVLRSFPPDAILFYIPQIVQALRYDKMGYVREYILWAASKSQLLAHQFIWNMKTNIYLDEEGHQKDPDIGDLLDQLVEEITGSLSGPAKDFYQREFDFFNKITNVSAIIKPYPKGDERKKACLSALSEVKVQPGCYLPSNPEAIVLDIDYKSGTPMQSAAKAPYLAKFKVKRCGVSELEKEGLRCRSDSEDECSTQEADGQKISWQAAIFKVGDDCRQDMLALQIIDLFKNIFQLVGLDLFVFPYRVVATAPGCGVIECIPDCTSRDQLGRQTDFGMYDYFTRQYGDESTLAFQQARYNFIRSMAAYSLLLFLLQIKDRHNGNIMLDKKGHIIHIDFGFMFESSPGGNLGWEPDIKLTDEMVMIMGGKMEATPFKWFMEMCVRGYLAVRPYMDAVVSLVTLMLDTGLPCFRGQTIKLLKHRFSPNMTEREAANFIMKVIQSCFLSNRSRTYDMIQYYQNDIPY |
分子量 | 123.4 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PIK4CA蛋白的3篇代表性文献摘要概览:
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1. **文献名称**:*Structural insights into the mechanism of human PI3Kα isoform-specific activation by phosphotyrosine peptides*
**作者**:Zhang, X., et al.
**摘要**:该研究解析了重组人PIK4CA蛋白(PI3Kα催化亚基)与调控亚基p85及磷酸化酪氨酸肽段的复合物晶体结构,揭示了PI3Kα在生长因子信号传导中的变构激活机制,为靶向PI3Kα的癌症药物设计提供了结构基础。
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2. **文献名称**:*Oncogenic mutations in PIK3CA lead to enhanced membrane recruitment and enzymatic activity*
**作者**:Burke, J.E., et al.
**摘要**:通过重组表达野生型和常见致癌突变体(如H1047R)的PIK4CA蛋白,结合脂质体结合实验和酶动力学分析,证明突变体因膜亲和力增加而导致PI3K通路过度激活,阐明了其在肿瘤发生中的作用机制。
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3. **文献名称**:*Development of a high-throughput assay for screening PIK4CA kinase inhibitors using recombinant protein*
**作者**:Wang, Y., et al.
**摘要**:本研究利用重组人PIK4CA蛋白建立了一种基于荧光共振能量转移(FRET)的高通量激酶活性检测平台,成功筛选出多个新型小分子抑制剂,为PI3Kα依赖性癌症的靶向治疗提供了候选化合物。
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**备注**:上述文献为虚拟示例,实际检索建议通过PubMed或Web of Science以关键词“recombinant PIK4CA protein”、“PI3Kα structure/function”等查询近年高影响力研究。
Recombinant human PIK3CA protein is derived from the PIK3CA gene, which encodes the p110α catalytic subunit of phosphatidylinositol 3-kinase (PI3K), a key enzyme in the PI3K/AKT/mTOR signaling pathway. This pathway regulates critical cellular processes, including growth, proliferation, survival, and metabolism. PIK3CA mutations are frequently observed in cancers (e.g., breast, colorectal, endometrial) and are linked to hyperactivation of PI3K, promoting uncontrolled cell growth and therapy resistance. Recombinant PIK3CA protein is produced using biotechnological methods, often expressed in mammalian or bacterial systems, to study its structure, enzymatic activity, and interaction with inhibitors. It typically retains functional domains, such as the kinase and regulatory domains, enabling researchers to explore mechanisms of oncogenic mutations (e.g., E545K, H1047R) that enhance lipid kinase activity. Applications include drug screening, structural studies for inhibitor design, and functional assays in cancer models. Its role in disease pathogenesis and therapeutic targeting underscores its importance in oncology research and precision medicine development.
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