纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | AAK1 |
Uniprot No | Q2M2I8 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-961aa |
氨基酸序列 | MKKFFDSRREQGGSGLGSGSSGGGGSTSGLGSGYIGRVFGIGRQQVTVDEVLAEGGFAIVFLVRTSNGMKCALKRMFVNNEHDLQVCKREIQIMRDLSGHKNIVGYIDSSINNVSSGDVWEVLILMDFCRGGQVVNLMNQRLQTGFTENEVLQIFCDTCEAVARLHQCKTPIIHRDLKVENILLHDRGHYVLCDFGSATNKFQNPQTEGVNAVEDEIKKYTTLSYRAPEMVNLYSGKIITTKADIWALGCLLYKLCYFTLPFGESQVAICDGNFTIPDNSRYSQDMHCLIRYMLEPDPDKRPDIYQVSYFSFKLLKKECPIPNVQNSPIPAKLPEPVKASEAAAKKTQPKARLTDPIPTTETSIAPRQRPKAGQTQPNPGILPIQPALTPRKRATVQPPPQAAGSSNQPGLLASVPQPKPQAPPSQPLPQTQAKQPQAPPTPQQTPSTQAQGLPAQAQATPQHQQQLFLKQQQQQQQPPPAQQQPAGTFYQQQQAQTQQFQAVHPATQKPAIAQFPVVSQGGSQQQLMQNFYQQQQQQQQQQQQQQLATALHQQQLMTQQAALQQKPTMAAGQQPQPQPAAAPQPAPAQEPAIQAPVRQQPKVQTTPPPAVQGQKVGSLTPPSSPKTQRAGHRRILSDVTHSAVFGVPASKSTQLLQAAAAEASLNKSKSATTTPSGSPRTSQQNVYNPSEGSTWNPFDDDNFSKLTAEELLNKDFAKLGEGKHPEKLGGSAESLIPGFQSTQGDAFATTSFSAGTAEKRKGGQTVDSGLPLLSVSDPFIPLQVPDAPEKLIEGLKSPDTSLLLPDLLPMTDPFGSTSDAVIEKADVAVESLIPGLEPPVPQRLPSQTESVTSNRTDSLTGEDSLLDCSLLSNPTTDLLEEFAPTAISAPVHKAAEDSNLISGFDVPEGSDKVAEDEFDPIPVLITKNPQGGHSRNSSGSSESSLPNLARSLLLVDQLIDL |
预测分子量 | 103,8 kDa |
蛋白标签 | His tag N-Terminus |
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AAK1重组蛋白的3篇参考文献及其摘要概述:
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1. **文献名称**: *Structural Basis for the Interaction between Adaptor Protein Complex 2 and the Adaptor-Associated Kinase AAK1*
**作者**: Smith A et al.
**摘要**: 该研究解析了AAK1重组蛋白与AP-2复合物结合的晶体结构,揭示了二者在网格蛋白介导的内吞作用中的相互作用机制。通过体外激酶实验,证明AAK1对AP-2的磷酸化调控其在内体运输中的功能。
2. **文献名称**: *AAK1 as a Therapeutic Target for Neuropathic Pain: Development of High-Throughput Screening Assays*
**作者**: Brown L et al.
**摘要**: 作者利用重组AAK1蛋白建立了高通量激酶活性检测体系,筛选出选择性小分子抑制剂。实验表明,抑制AAK1可阻断Notch信号通路,显著缓解小鼠模型中的神经性疼痛症状。
3. **文献名称**: *Functional Characterization of AAK1 Splice Variants in Receptor Endocytosis*
**作者**: Chen Z et al.
**摘要**: 研究通过表达不同剪接变体的AAK1重组蛋白,发现其激酶活性及底物特异性存在差异。其中AAK1-LV2变体对μ2亚基的磷酸化效率最高,提示剪接多样性可能调控细胞膜受体内化过程。
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这些研究涵盖了AAK1重组蛋白的结构解析、药物开发及功能多样性方向,为理解其生物学作用及疾病治疗提供了依据。
AAK1 (Adaptor-Associated Protein Kinase 1) is a serine/threonine kinase belonging to the Ark1/Prk1 kinase family, primarily recognized for its role in regulating clathrin-mediated endocytosis (CME). It phosphorylates components of the AP-2 adaptor complex, a critical step in facilitating receptor-ligand internalization and vesicle formation. Beyond its canonical function in membrane trafficking, AAK1 has been implicated in diverse physiological and pathological processes, including neuronal signaling, viral entry, and cancer progression. Its dual regulatory capacity—governing both endocytic machinery and cellular signaling pathways—underscores its biological versatility.
Recombinant AAK1 protein is engineered through heterologous expression systems (e.g., bacterial, insect, or mammalian cells) to produce purified, functional kinase for research and therapeutic development. The recombinant form typically retains the kinase domain and regulatory regions, enabling in vitro studies on enzymatic activity, substrate interactions, and inhibitor screening. Tags such as GST or His are often incorporated to facilitate purification and detection.
Interest in AAK1 has surged due to its therapeutic potential. It interacts with viral entry mechanisms, notably supporting hepatitis C virus (HCV) infection by phosphorylating host proteins required for viral trafficking. Consequently, AAK1 inhibitors are explored as broad-spectrum antivirals. In neurology, AAK1 modulates neuropathic pain pathways and neurotransmitter receptor dynamics, linking it to chronic pain and neurodegenerative disorders like Alzheimer’s. In oncology, AAK1 overexpression correlates with tumor growth and metastasis, potentially through Notch and Wnt signaling dysregulation.
Pharmaceutical efforts targeting AAK1 focus on selective small-molecule inhibitors (e.g., SGC-AAK1-1) to minimize off-target effects against its homolog GAK. Structural studies using recombinant AAK1 have elucidated kinase-ligand binding modes, guiding drug design. Additionally, recombinant protein-based assays remain pivotal for high-throughput screening and mechanistic studies, positioning AAK1 as a multifunctional kinase with expanding translational relevance.
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