PDF(Pubmed)
Abstract：
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.
摘要：
调节诱导邻近靶向嵌合体（RIPTAC），一类新的异双功能分子，在明确靶向和消除癌细胞，同时保持健康细胞不受伤害方面显示出希望。作为一种开创性的药物发现方法，RIPTAC通过与两种蛋白质形成稳定的复合物来工作，一种特别在癌细胞中发现的(靶蛋白，TP)和其他细胞存活所必需的(效应蛋白，EP),选择性破坏EP在癌细胞中的功能并导致细胞死亡。有趣的是,TP不需要与疾病进展有关，拓宽潜在药物靶点的范围。这篇综述总结了RIPTAC策略的发现和最新进展。此外,它讨论了该领域的相关机遇和挑战以及未来前景。
