Oprea Ioana, Smith Terry K
Biomedical Science Research Complex, Schools of Biology and Chemistry, University of Saint Andrews, North Haugh, St Andrews KY16 9ST, United Kingdom of Great Britain and Northern Ireland.
ACS Chem Biol. 2025 Jan 17;20(1):19-32. doi: 10.1021/acschembio.4c00608. Epub 2024 Dec 27.
Click chemistry is an immensely powerful technique for the synthesis of reliable and efficient covalent linkages. When undertaken in living cells, the concept is thereby coined bioorthogonal chemistry. Used in conjunction with the photo-cross-linking methodology, it serves as a sound strategy in the exploration of biological processes and beyond. Its broad scope has led to widespread use in many disciplines; however, this Review focuses on the use of click and bioorthogonal chemistry within medicinal chemistry, specifically with regards to drug development applications, namely, the use of DNA-encoded libraries as a novel technique for lead compound discovery, as well as the synthesis of antisense oligonucleotides and protein-drug conjugates. This Review aims to provide a critical perspective and a future outlook of this methodology, such as potential widespread use in cancer therapy and personalized medicine.
点击化学是一种用于合成可靠且高效共价键的极为强大的技术。当在活细胞中进行时，这一概念因而被称作生物正交化学。与光交联方法结合使用时，它是探索生物过程及其他领域的一种可靠策略。其广泛的应用范围已导致它在许多学科中得到广泛使用；然而，本综述聚焦于点击化学和生物正交化学在药物化学中的应用，特别是在药物开发应用方面，即使用DNA编码文库作为发现先导化合物的一种新技术，以及反义寡核苷酸和蛋白质 - 药物偶联物的合成。本综述旨在提供对该方法的批判性观点和未来展望，例如其在癌症治疗和个性化医学中潜在的广泛应用。
