研究动态
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RIPTAC(Rationalized Integrated Process for Targeted Active Components):一种突破性的药物发现方法。

RIPTACs: A groundbreaking approach to drug discovery.

发表日期:2023 Sep 19
作者: Zonghui Ma, Andrew A Bolinger, Jia Zhou
来源: DRUG DISCOVERY TODAY

摘要:

受调控的诱导亲近靶向嵌合物(RIPTACs)是一种新型异双功能分子,显示出特异性靶向和消除癌细胞的潜力,同时不伤害健康细胞。作为一种重大突破的药物开发方法,RIPTACs通过与两种蛋白质形成稳定的复合物来发挥作用,其中一种特异性地存在于癌细胞中(靶蛋白质,TP),另一种在细胞存活中普遍存在(效应蛋白质,EP),选择性地干扰癌细胞中EP的功能并引起细胞死亡。有趣的是,这些靶蛋白质与疾病进展无需关联,扩大了潜在药物靶点的范围。本综述总结了RIPTAC策略的发现和最新进展,同时讨论了相关机遇和挑战,并展望了该领域的未来前景。版权© 2023 Elsevier Ltd. 保留所有权利。
Regulated induced proximity targeting chimeras (RIPTACs), a new class of heterobifunctional molecules, show promise in specifically targeting and eliminating cancer cells while leaving healthy cells unharmed. As a groundbreaking drug discovery approach, RIPTACs work by forming a stable complex with two proteins, one specifically found in cancer cells (target protein, TP) and the other pan-essential for cell survival (effector protein, EP), selectively disrupting the function of the EP in cancer cells and causing cell death. Interestingly, the TPs need not be linked to disease progression, broadening the spectrum of potential drug targets. This review summarizes the discovery and recent advances of the RIPTAC strategy. Additionally, it discusses the associated opportunities and challenges as well as future perspectives in this field.Copyright © 2023 Elsevier Ltd. All rights reserved.