纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | PAK1 |
Uniprot No | Q13153 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-545aa |
氨基酸序列 | MSNNGLDIQDKPPAPPMRNTSTMIGAGSKDAGTLNHGSKPLPPNPEEKKKKDRFYRSILPGDKTNKKKEKERPEISLPSDFEHTIHVGFDAVTGEFTGMPEQWARLLQTSNITKSEQKKNPQAVLDVLEFYNSKKTSNSQKYMSFTDKSAEDYNSSNALNVKAVSETPAVPPVSEDEDDDDDDATPPPVIAPRPEHTKSVYTRSVIEPLPVTPTRDVATSPISPTENNTTPPDALTRNTEKQKKKPKMSDEEILEKLRSIVSVGDPKKKYTRFEKIGQGASGTVYTAMDVATGQEVAIKQMNLQQQPKKELIINEILVMRENKNPNIVNYLDSYLVGDELWVVMEYLAGGSLTDVVTETCMDEGQIAAVCRECLQALEFLHSNQVIHRDIKSDNILLGMDGSVKLTDFGFCAQITPEQSKRSTMVGTPYWMAPEVVTRKAYGPKVDIWSLGIMAIEMIEGEPPYLNENPLRALYLIATNGTPELQNPEKLSAIFRDFLNRCLEMDVEKRGSAKELLQHQFLKIAKPLSSLTPLIAAAKEATKNNH |
预测分子量 | 76.6kDa |
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3-4条关于PAK1重组蛋白的参考文献及其摘要内容:
---
1. **文献名称**:*"Regulation of PAK1 Activity and Autoinhibition by Phosphorylation and Dimerization"*
**作者**:Bokoch, G. M., et al.
**摘要**:该研究通过重组PAK1蛋白的表达和纯化,揭示了PAK1的自抑制机制及其通过磷酸化和二聚化调控激酶活性的分子机制,为PAK1在细胞信号转导中的动态调节提供了结构基础。
---
2. **文献名称**:*"Cloning and Expression of Active Recombinant PAK1 for Structural Studies"*
**作者**:Manser, E., & Leberer, E.
**摘要**:作者利用大肠杆菌表达系统成功克隆并纯化重组PAK1蛋白,结合X射线晶体学解析其活性构象,阐明了PAK1与Cdc42/Rac1结合后的构象变化及催化域激活机制。
---
3. **文献名称**:*"High-Throughput Screening of PAK1 Inhibitors Using Recombinant Kinase Domain"*
**作者**:Gao, Y., et al.
**摘要**:研究通过表达PAK1激酶结构域的重组蛋白,建立高通量筛选平台,鉴定出多个选择性小分子抑制剂,并验证其对肿瘤细胞迁移的抑制作用,为靶向PAK1的抗癌药物开发提供依据。
---
4. **文献名称**:*"Functional Analysis of PAK1 Mutants in Cancer Cell Invasion via Recombinant Protein Assays"*
**作者**:Kumar, R., & Vadlamudi, R. K.
**摘要**:通过构建PAK1突变体重组蛋白,研究其在体外激酶活性和细胞侵袭中的作用,发现关键磷酸化位点(如Ser144)的突变显著影响PAK1介导的细胞迁移和肿瘤转移。
---
这些文献涵盖了PAK1重组蛋白的制备、结构解析、功能研究和药物开发应用。如需具体文献来源(期刊、年份等),可进一步补充数据库检索信息(如PubMed ID)。
PAK1 (p21-activated kinase 1) is a serine/threonine protein kinase belonging to the PAK family, which plays critical roles in regulating cytoskeletal dynamics, cell proliferation, and survival. It is activated by binding to small GTPases Cdc42 and Rac1. serving as a downstream effector in Rho-family GTPase signaling pathways. PAK1 is widely expressed in various tissues and implicated in diverse cellular processes, including cell migration, apoptosis resistance, and gene transcription. Dysregulation of PAK1 has been linked to multiple diseases, particularly cancer, where its overexpression or hyperactivity promotes tumor invasion, metastasis, and therapeutic resistance. It also contributes to neurological disorders, immune responses, and cardiovascular pathologies.
Recombinant PAK1 proteins are engineered using expression systems (e.g., E. coli, insect, or mammalian cells) to produce purified, functional kinase domains or full-length forms for research. These proteins retain catalytic activity and binding capacity, enabling in vitro studies on kinase-substrate interactions, signaling mechanisms, and inhibitor screening. Common variants include wild-type, constitutively active (e.g., T423E mutation), and kinase-dead mutants (e.g., K299R) to dissect activation mechanisms. Tags like GST, His, or FLAG are often fused for purification and detection. Applications range from structural analysis (e.g., crystallography) to drug discovery, where PAK1 inhibitors are explored for anticancer therapies. Its role in cross-talk with pathways like MAPK, PI3K/AKT, and Wnt underscores its relevance as a therapeutic target and research tool.
×