Turku Bioscience Centre, University of Turku and Åbo Akademi University, Tykistökatu 6, 20520, Turku, Finland.
Sci Rep. 2024 May 15;14(1):11174. doi: 10.1038/s41598-024-61337-3.
Current treatments for anxiety and depression show limited efficacy in many patients, indicating the need for further research into the underlying mechanisms. JNK1 has been shown to regulate anxiety- and depressive-like behaviours in mice, however the effectors downstream of JNK1 are not known. Here we compare the phosphoproteomes from wild-type and Jnk1-/- mouse brains and identify JNK1-regulated signalling hubs. We next employ a zebrafish (Danio rerio) larvae behavioural assay to identify an antidepressant- and anxiolytic-like (AA) phenotype based on 2759 measured stereotypic responses to clinically proven antidepressant and anxiolytic (AA) drugs. Employing machine learning, we classify an AA phenotype from extracted features measured during and after a startle battery in fish exposed to AA drugs. Using this classifier, we demonstrate that structurally independent JNK inhibitors replicate the AA phenotype with high accuracy, consistent with findings in mice. Furthermore, pharmacological targeting of JNK1-regulated signalling hubs identifies AKT, GSK-3, 14-3-3 ζ/ε and PKCε as downstream hubs that phenocopy clinically proven AA drugs. This study identifies AKT and related signalling molecules as mediators of JNK1-regulated antidepressant- and anxiolytic-like behaviours. Moreover, the assay shows promise for early phase screening of compounds with anti-stress-axis properties and for mode of action analysis.
目前治疗焦虑和抑郁的方法在许多患者中显示出有限的疗效,这表明需要进一步研究其潜在机制。JNK1 已被证明可调节小鼠的焦虑和抑郁样行为,但 JNK1 的下游效应物尚不清楚。在这里,我们比较了野生型和 Jnk1-/-小鼠大脑的磷酸化蛋白质组,并确定了 JNK1 调节的信号枢纽。接下来,我们利用斑马鱼(Danio rerio)幼虫行为测定法,根据 2759 个对临床证实的抗抑郁药和抗焦虑药(AA)药物的刻板反应来识别抗抑郁药和抗焦虑药(AA)表型。通过机器学习,我们从暴露于 AA 药物的鱼在开始电池期间和之后测量的提取特征中分类 AA 表型。使用这个分类器,我们证明了结构上独立的 JNK 抑制剂以高精度复制 AA 表型,与小鼠中的发现一致。此外,针对 JNK1 调节的信号枢纽的药理学靶向确定 AKT、GSK-3、14-3-3 ζ/ε 和 PKCε 作为与临床证实的 AA 药物类似的下游枢纽。这项研究确定了 AKT 和相关信号分子作为 JNK1 调节的抗抑郁药和抗焦虑样行为的介质。此外,该测定法有望用于具有抗应激轴特性的化合物的早期筛选以及作用模式分析。