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光控PROTAC研究进展

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蛋白水解靶向嵌合体(PROTAC)作为一种小分子工具,可以选择性地诱导目标蛋白质降解,被认为是控制细胞内蛋白质水平的有力工具.然而,PROTAC潜在的脱靶效应是阻碍其临床应用的主要因素之一.最近,已经有多个课题组将光作为额外刺激来控制诱导蛋白质降解.本文作者就光控PROTAC的设计原理和研究进展进行梳理总结,并讨论了光控降解蛋白质的不足与未来发展,以期为光控PROTAC进一步研究提供参考.
Research progress on light-controllable PROTAC
As a small molecule tool that selectively induces the degradation of target proteins,PROTAC is considered as a powerful tool for controlling intracellular protein levels.However,the potential off-target effect of PROTAC is one of the major limiting factors hindering its clinical application.Recently,several research groups have utilized light as an additional stimulus to control induced protein degradation.This paper reviews the design principles and research progress of light-controlled PROTAC,discusses the limitations and future developments of light-controlled protein degradation,aiming to provide insights for further research on light-controlled PROTAC.

PROTACE3 ubiquitin-ligaselight-induced protein degradationdegrader

肖文轩、杨艳平、于泽洋、白俊

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西安医学院研究生工作部,陕西西安 710021

陕西省人民医院肿瘤内科,陕西西安 710068

蛋白水解靶向嵌合体 E3泛素连接酶 光诱导蛋白质降解 降解剂

2024

中国药物化学杂志
沈阳药科大学,中国药学会

中国药物化学杂志

CSTPCD
影响因子:0.463
ISSN:1005-0108
年,卷(期):2024.34(6)