AAK1靶点的成药性连接蛋白相关激酶1 (AAK1)是治疗神经性疼痛的可行靶点，这在小鼠敲除表型中首次得到证实。 AAK1为 丝氨酸 /苏氨酸激酶的Arkl/Prkl家族的成员，且已被鉴定为PC12细胞中神经调节蛋白- l/ErbB4信号传导的抑制剂。 经由RNA干扰介导的基因沉默或用激酶抑制剂K252a (其抑制AAK1激酶活性)处理使AAK1表达丧失导致神经调节蛋白-1诱导的神经突过度增生的增强。 这些处理导致ErbB4表达增加和ErbB4在质膜中或在质膜附近累积增加。 NRG1和ErbB4中 …

2024年12月24日 · AAK1 (AP2 Associated Kinase 1) is a Protein Coding gene. Diseases associated with AAK1 include Rabies and Hepatitis C Virus. Among its related pathways are Vesicle-mediated transport and Clathrin-mediated endocytosis.

Adaptor-associated protein kinase 1 also known as AP2-associated protein kinase 1 is an enzyme that in humans is encoded by the AAK1 gene [5] [6] [7] and is involved in clathrin mediated endocytosis. Alternatively spliced transcript variants have been described, but their biological validity has not been determined.

2024年3月20日 · TIM-098a could inhibit AAK1 activity in transfected cultured cells (IC 50 = 0.87 µM), indicating cell-membrane permeability of the compound. Overexpression of AAK1 in HeLa cells significantly...

2022年7月7日 · AAK1是调控AP-2蛋白μ2亚基 (AP2M1) 第156位苏氨酸 (T156) 磷酸化的特异性关键激酶。AAK1介导的AP-2蛋白μ2亚基磷酸化能够确保AP-2蛋白对货物膜蛋白分选信号的高亲和力。该位点被磷酸化后, 有利于μ2亚基保持开放构象, 便于其与质膜结构结合 [22]。由此可见, 在CME过程中, AP-2蛋白μ2亚基T156的磷酸化水平高低决定了CME过程的顺利进行。因此, AAK1对CME过程起着至关重要的作用。

Adaptor associated kinase 1 (AAK1), a member of the Ark1/Prk1 family of Ser/Thr kinases, is a specific key kinase regulating Thr156 phosphorylation at the μ2 subunit of the adapter complex-2 (AP-2) protein.

随后，在细胞内过表达aak1，发现细胞内整体翻译水平上升（图4c），而干扰aak1后整体翻译水平下降（图4d），提示aak1可以正向调控细胞内整体翻译水平。

Here we identify and characterize a novel member of the Prk/Ark family of serine/threonine kinases, adaptor-associated kinase (AAK)1. We find that AAK1 copurifies with adaptor protein (AP)2 and that it directly binds the ear domain of α-adaptin in vivo and in vitro.

2023年2月15日 · Adaptor-Associated Kinase 1 (AAK1), a Ser/Thr protein kinase, responsible for regulating clathrin-mediated endocytosis, is ubiquitous in the central nervous system (CNS). AAK1 plays an important role in neuropathic pain and a variety of other human diseases, including viral invasion, Alzheimer's dis …

2016年7月16日 · Using a nonbrain-penetrant AAK1 inhibitor and local administration of an AAK1 inhibitor, the relevant pool of AAK1 for antineuropathic action was found to be in the spinal cord. Consistent with these results, AAK1 inhibitors dose-dependently reduced the increased spontaneous neural activity in the spinal cord caused by CCI and blocked the ...