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小分子JAK2抑制剂的最新进展与未来展望

Recent advances and future perspectives in small molecule JAK2 inhibitors.

作者信息

Yasir Muhammad, Choe Jongseon, Hassan Mubashir, Kloczkowski Andrzej, Chun Wanjoo

机构信息

Department of Pharmacology, Kangwon National University School of Medicine, Chuncheon, Republic of Korea.

Department of Microbiology and Immunology, Kangwon National University School of Medicine, Chuncheon, Republic of Korea.

出版信息

Future Med Chem. 2025 May;17(10):1175-1191. doi: 10.1080/17568919.2025.2507564. Epub 2025 May 20.

Abstract

The Janus kinase (JAK)/Signal Transducer and Activator of Transcription (STAT) signaling pathway is essential for controlling immune function, blood cell formation, and cell growth. Dysregulation of this pathway is implicated in various diseases, including hematologic malignancies, autoimmune disorders, and chronic inflammatory conditions. This review provides a comprehensive overview of the structural and functional aspects of JAK/STAT signaling, with a particular focus on the role of JAK2. This manuscript explores the primary regulators of the JAK/STAT pathway, such as Suppressors Of Cytokine Signaling (SOCS), Protein Inhibitors of Activated STATs (PIAS), and Protein Tyrosine Phosphatases (PTPs), which play a crucial role in maintaining cellular balance and stability. Additionally, the therapeutic landscape of JAK2 inhibitors is explored, covering both approved and investigational drugs, including their mechanisms of action, efficacy, and safety profiles. Emerging strategies such as drug repositioning using computational approaches and experimental validation are also highlighted. By integrating insights from molecular docking studies, machine learning models, and kinase assays, this review emphasizes the potential of JAK2 inhibitors in disease management.

摘要

Janus激酶(JAK)/信号转导子与转录激活子(STAT)信号通路对于控制免疫功能、血细胞生成和细胞生长至关重要。该通路的失调与多种疾病有关,包括血液系统恶性肿瘤、自身免疫性疾病和慢性炎症性疾病。本综述全面概述了JAK/STAT信号传导的结构和功能方面,特别关注JAK2的作用。本文探讨了JAK/STAT通路的主要调节因子,如细胞因子信号抑制因子(SOCS)、活化STAT蛋白抑制剂(PIAS)和蛋白酪氨酸磷酸酶(PTP),它们在维持细胞平衡和稳定性方面起着关键作用。此外,还探讨了JAK2抑制剂的治疗前景,涵盖已批准和正在研究的药物,包括它们的作用机制、疗效和安全性。还强调了使用计算方法和实验验证进行药物重新定位等新兴策略。通过整合分子对接研究、机器学习模型和激酶分析的见解,本综述强调了JAK2抑制剂在疾病管理中的潜力。

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