一种新兴的治疗工具——PROTACOA
The Emergence of a Novel Therapeutic Modality—PROTAC
蛋白降解靶向嵌合体(PROTAC)技术是一种新兴的药物研发手段,自2001 年首次被提出以来,已经在药物研发领域取得了显著的进展.其基本原理是利用细胞内的泛素-蛋白酶体系统,通过特定的双功能小分子诱导目标蛋白质的泛素化和随后的降解.近年来,随着研究的深入和临床实验的推进,多款基于PROTAC技术的药物进入了临床阶段,并且显示出良好的疗效和安全性.本文将从PROTAC技术降解机制、常见的PROTAC分子,以及PROTAC技术的优势和未来发展趋势等方面做简要介绍,希望为其今后的研究和临床应用提供参考.
The technology of proteolysis-targeting chimera(PROTAC)represents a pioneering approach in drug development,having achieved significant advancements since its inception in 2001.Its fundamental principle involves leveraging the ubiquitin-proteasome system within cells to induce the ubiquitination and subsequent degradation of target proteins through specific bifunctional small molecules.In recent years,with the deepening of research and the advancement of clinical trials,several drugs based on PROTAC have entered the clinical stage,demonstrating favorable efficacy and safety profiles.This article aims to provide a concise overview of the degradation mechanism of PROTAC,common PROTAC molecules,as well as the advantages and future trends of PROTAC technology,providing reference for future research and clinical applications.
沈继伟;张敬泽;傅浩栋;杨睿;周云鹏
辽宁大学 药学院,辽宁 沈阳 110036||辽宁省小分子靶向药物研发工程研究中心,辽宁 沈阳 110036辽宁大学 药学院,辽宁 沈阳 110036辽宁大学 药学院,辽宁 沈阳 110036辽宁大学 药学院,辽宁 沈阳 110036辽宁大学 药学院,辽宁 沈阳 110036||辽宁省小分子靶向药物研发工程研究中心,辽宁 沈阳 110036
医药卫生
蛋白降解靶向嵌合体泛素-蛋白酶体降解剂发展趋势
proteolysis-targeting chimeraubiquitin-proteasomedegrading agentdevelopment trend
《辽宁大学学报（自然科学版）》 2026 (1)
72-79,8
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