治疗成像技术因其实时诊断癌症和有效治疗的能力而受到广泛关注。通过共价连接影像剂、治疗剂、刺激响应连接物和/或靶向分子，可合成可活化双功能分子剂量。它们可以通过肿瘤部位过度表达的生理刺激或外部触发器进行选择性激活，释放影像剂和细胞毒性药物，从而为肿瘤成像和治疗提供许多优势，如高信噪比、低系统毒性和改善的治疗效果。本综述总结了对各种生理或外部刺激响应的双功能分子剂量用于癌症治疗成像技术的最新进展。详细阐述了这些分子剂的分子设计、合成策略、可激活机制和生物医学应用，并对该领域的挑战和机遇进行了简要讨论。 版权所有 © 2023 Elsevier B.V. 出版

Theranostics has attracted great attention due to its ability to combine the real-time diagnosis of cancers with efficient treatment modalities. Activatable dual-functional molecular agents could be synthesized by covalently conjugating imaging agents, therapeutic agents, stimuli-responsive linkers and/or targeting molecules together. They could be selectively activated by overexpressed physiological stimuli or external triggers at the tumor sites to release imaging agents and cytotoxic drugs, thus offering many advantages for tumor imaging and therapy, such as a high signal-to-noise ratio, low systemic toxicity, and improved therapeutic effects. This review summarizes the recent advances of dual-functional molecular agents that respond to various physiological or external stimuli for cancer theranostics. The molecular designs, synthetic strategies, activatable mechanisms, and biomedical applications of these molecular agents are elaborated, followed by a brief discussion of the challenges and opportunities in this field.Copyright © 2023. Published by Elsevier B.V.