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点击化学在癌症治疗先进技术中的印记。

Signature of click chemistry in advanced techniques for cancer therapeutics.

作者信息

Ragab Sherif Shaban

机构信息

Photochemistry Department, Chemical Industries Research Institute, National Research Centre El-Buhouth St, P.O. 12622, Dokki Giza Egypt

出版信息

RSC Adv. 2025 Apr 4;15(14):10583-10601. doi: 10.1039/d5ra01196e.

DOI:10.1039/d5ra01196e
PMID:40190630
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11970365/
Abstract

Click chemistry has made a revolution in the field of chemical biology owing to its high efficiency, specificity, and mild reaction conditions. The copper(i)-catalyzed azide-alkyne cycloaddition (CuAAC) and strain-promoted [3 + 2] azide-alkyne cycloaddition (SPAAC) stand out as the most popular click reactions that construct a stable triazole ring by reacting an azide with an alkyne. These two reactions represent an ideal choice for biological applications due to its specificity, reliability, and biocompatibility. As a powerful modular synthetic approach for creating new molecular entities, it has seen increasing use in anticancer drug discovery. The present "state of the art" focuses mainly on the signature of click chemistry (CuAAC and SPAAC) in advanced techniques for cancer therapeutics, which includes cancer immunotherapy, antibody-drug conjugates, development of proteolysis-targeting chimeras, targeted dual-agent combination therapy for cancer, exosome modification for cancer therapy, and photodynamic therapy (PDT).

摘要

点击化学因其高效性、特异性和温和的反应条件，在化学生物学领域引发了一场革命。铜（I）催化的叠氮化物-炔烃环加成反应（CuAAC）和应变促进的[3+2]叠氮化物-炔烃环加成反应（SPAAC）是最受欢迎的点击反应，它们通过使叠氮化物与炔烃反应构建稳定的三唑环。由于其特异性、可靠性和生物相容性，这两种反应是生物应用的理想选择。作为一种创建新分子实体的强大模块化合成方法，它在抗癌药物发现中的应用越来越多。目前的“最新技术水平”主要集中在点击化学（CuAAC和SPAAC）在癌症治疗先进技术中的应用，包括癌症免疫疗法、抗体-药物偶联物、蛋白酶靶向嵌合体的开发、癌症的靶向双药联合治疗、用于癌症治疗的外泌体修饰以及光动力疗法（PDT）。

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本文引用的文献

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Anticancer Tetranuclear Cu(I) Complex Catalyzes a Click Reaction to Synthesize a Chemotherapeutic Agent in situ to Achieve Targeted Dual-Agent Combination Therapy for Cancer.抗癌四核铜（I）配合物催化点击反应原位合成化疗药物，实现癌症的靶向双药联合治疗。
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Recent advances in triazole synthesis via click chemistry and their pharmacological applications: A review.点击化学法合成三氮唑及其药理学应用的最新进展：综述。
Bioorg Med Chem Lett. 2024 Nov 1;112:129927. doi: 10.1016/j.bmcl.2024.129927. Epub 2024 Aug 15.
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Protein click chemistry and its potential for medical applications.
蛋白质点击化学及其在医学应用中的潜力。
Q Rev Biophys. 2024 Apr 15;57:e6. doi: 10.1017/S0033583524000027.
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Global cancer statistics 2022: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries.2022 年全球癌症统计数据：全球 185 个国家和地区 36 种癌症的发病率和死亡率全球估计数。
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