State Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, University of Science and Technology of China, Changchun, 130022, China.
Angew Chem Int Ed Engl. 2021 Mar 8;60(11):5626-5643. doi: 10.1002/anie.201914511. Epub 2020 Oct 13.
Severe side effects and poor therapeutic efficacy are the main drawbacks of current anticancer drugs. These problems can be mitigated by targeting, but the targeting efficacy of current drugs is poor and urgently needs improvement. Taking this into consideration, this Review first summarizes the current targeting strategies for cancer therapy in terms of cancer tissue and organelles. Then, we analyse the systematic targeting of anticancer drugs and conclude that a typical journey for a targeted drug administered by intravenous injection is a CTIO cascade of at least four steps. Furthermore, to ensure high overall targeting efficacy, the properties of a targeting drug needed in each step are further analysed, and some guidelines for structure optimization to obtain effective targeting drugs are offered. Finally, some viewpoints highlighting the crucial problems and potential challenges of future research on targeted cancer therapy are presented. This review could actively promote the development of precision medicine against cancer.
严重的副作用和较差的治疗效果是当前抗癌药物的主要缺点。通过靶向治疗可以减轻这些问题，但目前药物的靶向效果较差，急需改进。有鉴于此，本文首先从癌症组织和细胞器的角度总结了当前癌症治疗的靶向策略。然后，我们分析了抗癌药物的系统靶向作用，并得出结论，静脉注射给药的靶向药物的典型旅程至少要经过 CTIO 级联的四个步骤。此外，为了确保高的整体靶向效果，进一步分析了靶向药物在每个步骤中所需的特性，并提供了一些结构优化的指导原则，以获得有效的靶向药物。最后，提出了一些观点，强调了靶向癌症治疗未来研究的关键问题和潜在挑战。本文的综述将积极推动癌症精准医学的发展。
