创新链/学科链/研发链/产业链

新药研发前沿动态 / 医药领域趋势进展

分子伴侣HSP90的抑制策略分析及最新进展

Analysis and Recent Progress of Inhibition Strategies for the Molecular Chaperone HSP90

  • 摘要: 分子伴侣热休克蛋白(heat shock protein,HSP)90在蛋白质折叠、细胞信号传导及细胞稳态维持中发挥关键作用。其功能异常与肿瘤等多种疾病的发生发展密切相关,使其成为药物开发领域的重要靶标。综述HSP90抑制策略的演变历程及最新研究进展,将已报道的HSP90小分子抑制剂系统划分为4代并进行全面总结。通过详细阐述各代抑制剂代表性分子的设计策略、化学结构特征及作用机制,深入分析当前HSP90抑制剂研发中存在的核心问题,同时对未来的研究方向进行展望,旨在为靶向HSP90的小分子抑制剂设计提供科学思路与研究启发。

     

    Abstract: The molecular chaperone heat shock protein (HSP)90 plays a crucial role in protein folding, cell signal transduction, and maintenance of cellular homeostasis. Its dysfunction is closely related to the occurrence and development of various diseases such as tumors, making it an important target in the field of drug development. This article reviews the evolution of HSP90 inhibition strategies and the latest research progress, and systematically classifies the reported small molecule HSP90 inhibitors into 4 generations for a comprehensive summary. By elaborating on the design strategies, chemical structure characteristics, and action mechanisms of representative molecules of each generation of inhibitors, it analyzes in depth the core issues existing in the current research and development of HSP90 inhibitors, with a prospect of the future research directions, aiming to provide scientific ideas and research inspiration for the design of small molecule inhibitors targeting HSP90.

     

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