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GAS6-AXL 复合物的内吞运输与持续的 AKT 激活有关。

Endocytic trafficking of GAS6-AXL complexes is associated with sustained AKT activation.

机构信息

Laboratory of Cell Biology, International Institute of Molecular and Cell Biology, Warsaw, Poland.

出版信息

Cell Mol Life Sci. 2022 May 27;79(6):316. doi: 10.1007/s00018-022-04312-3.

Abstract

AXL, a TAM receptor tyrosine kinase (RTK), and its ligand growth arrest-specific 6 (GAS6) are implicated in cancer metastasis and drug resistance, and cellular entry of viruses. Given this, AXL is an attractive therapeutic target, and its inhibitors are being tested in cancer and COVID-19 clinical trials. Still, astonishingly little is known about intracellular mechanisms that control its function. Here, we characterized endocytosis of AXL, a process known to regulate intracellular functions of RTKs. Consistent with the notion that AXL is a primary receptor for GAS6, its depletion was sufficient to block GAS6 internalization. We discovered that upon receptor ligation, GAS6-AXL complexes were rapidly internalized via several endocytic pathways including both clathrin-mediated and clathrin-independent routes, among the latter the CLIC/GEEC pathway and macropinocytosis. The internalization of AXL was strictly dependent on its kinase activity. In comparison to other RTKs, AXL was endocytosed faster and the majority of the internalized receptor was not degraded but rather recycled via SNX1-positive endosomes. This trafficking pattern coincided with sustained AKT activation upon GAS6 stimulation. Specifically, reduced internalization of GAS6-AXL upon the CLIC/GEEC downregulation intensified, whereas impaired recycling due to depletion of SNX1 and SNX2 attenuated AKT signaling. Altogether, our data uncover the coupling between AXL endocytic trafficking and AKT signaling upon GAS6 stimulation. Moreover, our study provides a rationale for pharmacological inhibition of AXL in antiviral therapy as viruses utilize GAS6-AXL-triggered endocytosis to enter cells.

摘要

AXL 是一种 TAM 受体酪氨酸激酶(RTK)及其配体生长停滞特异性基因 6(GAS6)与癌症转移和耐药性以及病毒的细胞进入有关。鉴于此,AXL 是一个有吸引力的治疗靶点,其抑制剂正在癌症和 COVID-19 临床试验中进行测试。尽管如此,人们对控制其功能的细胞内机制知之甚少。在这里,我们描述了 AXL 的内吞作用,这一过程已知可调节 RTKs 的细胞内功能。与 AXL 是 GAS6 的主要受体的观点一致,其耗竭足以阻止 GAS6 的内化。我们发现,在受体结合后,GAS6-AXL 复合物通过多种内吞途径(包括网格蛋白介导和非网格蛋白依赖途径)被快速内化,在后一种途径中,CLIC/GEEC 途径和巨胞饮作用。AXL 的内化严格依赖于其激酶活性。与其他 RTKs 相比,AXL 的内化速度更快,并且大部分内化的受体不会被降解,而是通过 SNX1 阳性内体被回收。这种运输模式与 GAS6 刺激后 AKT 的持续激活一致。具体而言,CLIC/GEEC 下调后 GAS6-AXL 内化减少,而 SNX1 和 SNX2 耗竭导致的回收受损则减弱了 AKT 信号。总之,我们的数据揭示了 GAS6 刺激下 AXL 内吞运输和 AKT 信号之间的耦合。此外,我们的研究为抗病毒治疗中 AXL 的药理学抑制提供了依据,因为病毒利用 GAS6-AXL 触发的内吞作用进入细胞。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0117/11071716/6c2d22d5d6f5/18_2022_4312_Fig1_HTML.jpg

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