在过去的十年中，发现新型癌症治疗方案引起了极大的兴趣。在这方面，多药物耐药性（MDR）是癌症治疗的主要挑战。癌细胞越来越能够通过采用不同的机制对现有化疗药物产生抗药性，凸显了发现克服MDR的方法的重要性。一种有前途的策略是利用寡核苷酸（aptamers）作为独特的工具来针对耐药机制中的元素或信号，或开发活性靶向药物输送系统或嵌合物，从而使新型药物精确地传递以抑制常规上难以制药的抗药性元素。此外，由于它们相对于蛋白质同源物具有的优势，特别是改善了的靶向作用、增强的热稳定性、更容易生产和更优越的肿瘤穿透性，寡核苷酸正在崛起，并经常被考虑用于开发癌症治疗。在这里，我们强调了显著的耐药通路，并深入讨论使用寡核苷酸作为克服癌症MDR的前景性工具。 版权©2023年Elsevier B.V. 发布。

Discovering novel cancer therapies has attracted extreme interest in the last decade. In this regard, multidrug resistance (MDR) to chemotherapies is the primary challenge in cancer treatment. Cancerous cells are growingly become resistant to existing chemotherapeutics by employing diverse mechanisms, highlighting the significance of discovering approaches to overcome MDR. One promising strategy is utilizing aptamers as unique tools to target elements or signalings incorporated in resistance mechanisms or develop active targeted drug delivery systems or chimeras enabling the precise delivery of novel agents to inhibit the conventionally undruggable resistance elements. Further, due to their advantages over their proteinaceous counterparts, particularly antibodies, including improved targeting action, enhanced thermal stability, easier production, and superior tumor penetration, aptamers are emerging and have frequently been considered for developing cancer therapeutics. Here, we highlighted significant chemoresistance pathways and thoroughly discussed using aptamers as prospective tools to surmount cancer MDR.Copyright © 2023. Published by Elsevier B.V.