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JNK抑制剂开发的进展:在神经退行性疾病和纤维化中的治疗前景

Advances in JNK inhibitor development: therapeutic prospects in neurodegenerative diseases and fibrosis.

作者信息

Bhujbal Swapnil P, Hah Jung-Mi

机构信息

College of Pharmacy, Hanyang University, Ansan, 15588, Republic of Korea.

Institute of Pharmaceutical Science and Technology, Hanyang University, ANSAN, 15588, Republic of Korea.

出版信息

Arch Pharm Res. 2025 Sep 8. doi: 10.1007/s12272-025-01566-w.

Abstract

c-Jun N-terminal kinases (JNKs), a subfamily of mitogen-activated protein kinases (MAPKs), are key mediators of cellular responses to environmental stress, inflammation, and apoptotic signals. The three isoforms-JNK1, JNK2, and JNK3 exhibit both overlapping and isoform-specific functions. While JNK1 and JNK2 are broadly expressed across tissues and regulate immune signaling, cell proliferation, and apoptosis, JNK3 expression is largely restricted to the brain, heart, and testis, where it plays a crucial role in neuronal function and survival. Subtle structural variations among the isoforms, particularly within the ATP-binding pocket and activation loop, provide a basis for the developing isoform-selective inhibitors to improve therapeutic precision. JNK3 has been increasingly recognized for its involvement in the pathogenesis of neurodegenerative disorders, including Alzheimer's and Parkinson's diseases, through mechanisms involving neuroinflammation, oxidative stress, and neuronal apoptosis. Given the limited efficacy of current therapies, which remain largely symptomatic and do not modify disease progression, covalent inhibitors of JNK3 represent a compelling alternative due to their potential for high selectivity and sustained target engagement. In parallel, JNK signaling contributes to fibrosis, with JNK1 serving as the predominant isoform driving profibrotic pathways such as fibroblast activation and extracellular matrix (ECM) deposition. Current antifibrotic agents provide only partial benefit and lack specificity for downstream effectors like JNK1. PROteolysis TArgeting Chimeras (PROTACs), which induce selective protein degradation via the ubiquitin-proteasome system, represent a promising modality to overcome these limitations. Selective degradation of JNK1 could provide a novel therapeutic avenue for fibrotic diseases. This review highlights therapeutic efforts to date and discusses how emerging approaches-particularly covalent JNK3 inhibitors for neurodegeneration and PROTACs for JNK1 in fibrosis-may advance future treatment paradigms.

摘要

c-Jun氨基末端激酶(JNKs)是丝裂原活化蛋白激酶(MAPKs)的一个亚家族,是细胞对环境应激、炎症和凋亡信号作出反应的关键介质。三种异构体——JNK1、JNK2和JNK3表现出重叠和异构体特异性功能。虽然JNK1和JNK2在各组织中广泛表达并调节免疫信号传导、细胞增殖和凋亡,但JNK3的表达主要局限于脑、心脏和睾丸,在这些组织中它在神经元功能和存活中起关键作用。异构体之间细微的结构差异,特别是在ATP结合口袋和激活环内的差异,为开发异构体选择性抑制剂以提高治疗精准度提供了基础。JNK3因其通过涉及神经炎症、氧化应激和神经元凋亡的机制参与神经退行性疾病(包括阿尔茨海默病和帕金森病)的发病过程而越来越受到认可。鉴于目前疗法的疗效有限,这些疗法在很大程度上仍只是缓解症状,无法改变疾病进展,JNK3的共价抑制剂因其具有高选择性和持续靶向作用的潜力而成为一种有吸引力的替代方案。同时,JNK信号传导促进纤维化,JNK1是驱动成纤维细胞活化和细胞外基质(ECM)沉积等促纤维化途径的主要异构体。目前的抗纤维化药物仅提供部分益处,并且对JNK1等下游效应器缺乏特异性。蛋白酶靶向嵌合体(PROTACs)通过泛素-蛋白酶体系统诱导选择性蛋白质降解,是克服这些局限性的一种有前景的方式。选择性降解JNK1可为纤维化疾病提供一种新的治疗途径。本综述重点介绍了迄今为止的治疗努力,并讨论了新兴方法——特别是用于神经退行性疾病的共价JNK3抑制剂和用于纤维化的JNK1的PROTACs——如何推动未来的治疗模式。

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