Chemical reactions that can proceed in living systems while not interfering with native biochemical processes are collectively referred to as bioorthogonal chemistry. Selectivity, efficiency, and aqueous compatibility are three significant characteristics of an ideal bioorthogonal reaction. To date, the specialized bioorthogonal reactions that have been reported include: Cu (I)-catalyzed [3 + 2] azido- alkyne cycloadditions (CuAAC), strain-promoted [3 + 2] azide-alkyne cycloadditions (SPAAC), Staudinger ligation, photo-click 1,3-dipolar cycloadditions, strain-promoted alkyne-nitrone cycloadditions (SPANC), transition metal catalysis (TMC), and inverse electron demand Diels-Alder (IEDDA). These reactions are divided into two subtypes, 1) bond-formation reactions (e.g. CuAAC, SPAAC, photo-click cycloadditions, SPANC), which can be conventionally applied in the chemical biology field for target identification, protein-specific modifications and others; and 2) bond-release reactions (e.g. Staudinger ligation, TMC, and IEDDA), which are emerging as powerful approaches for the study of protein activation and drug discovery. Over the past decade, bioorthogonal chemistry has enabled important compound design features in targeted drug discovery and has expanded biological knowledge on intractable targets. Research groups have also focused on the discovery of reactions with improved biocompatibility and increased reaction rates, which will undoubtably prove essential for future therapeutic development. Herein, we highlight two significant applications of bioorthogonal chemistry to drug discovery, which are tumor-targeted prodrug delivery and activation, and self-assembly of bifunctional molecules. The relevant challenges and opportunities are also discussed.

Gang Liu

Eric A. Wold

Jia Zhou

Current Topics in Medicinal Chemistry

CURRENT TOPICS IN MEDICINAL CHEMISTRY 是一个论坛，用于审查药物化学家和相关学科的其他人感兴趣的领域。每期仅针对特定主题，包含 6 到 9 篇评论，为读者提供对该领域的全面调查。一位特邀编辑，他是所审查主题的专家，将汇编每一期。药物化学当前主题的范围将涵盖药物化学的所有领域，包括合理药物设计、合成化学、生物有机化学、高通量筛选、组合化学、化合物多样性测量、药物吸收、药物分布、代谢、新的和新兴的药物靶点、天然产物、药物基因组学和构效关系。药物化学是一门迅速成熟的学科。研究结构和功能之间的关系对于理解生命的分子基础是绝对必要的。药物化学的当前主题旨在促进科学知识和洞察力的增长，并促进新治疗剂的发现和开发，以治疗使人衰弱的人类疾病。对于希望随时了解最新和最重要进展的每一位药物化学家来说，该杂志都是必不可少的。

Current Topics in Medicinal Chemistry is a forum dedicated to reviewing areas of interest for medicinal chemists and others in related disciplines. Each issue focuses on a specific topic and contains 6 to 9 review articles, providing readers with a comprehensive survey of the field. Each issue is compiled by a guest editor who is an expert in the reviewed topic. The scope of Current Topics in Medicinal Chemistry encompasses all areas of medicinal chemistry, including rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurement, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly evolving discipline, and understanding the relationship between structure and function is essential for grasping the molecular basis of life. The aim of Current Topics in Medicinal Chemistry is to foster the growth of scientific knowledge and insights and to facilitate the discovery and development of new therapeutic agents to combat debilitating human diseases. This journal is indispensable for every medicinal chemist who wishes to stay updated on the latest and most significant advancements.

《Current Topics in Medicinal Chemistry》是一个专门审查药物化学及相关学科领域的论坛。每期围绕特定主题，包含6到9篇评论文章，为读者提供该领域的全面调查。每一期由一位特邀编辑负责，他是所审查主题的专家。该期刊涵盖药物化学的各个领域，包括合理药物设计、合成化学、生物有机化学、高通量筛选、组合化学、化合物多样性测量、药物吸收、药物分布、代谢、新的和新兴的药物靶点、天然产物、药物基因组学和构效关系。药物化学是一门迅速发展的学科，研究结构与功能之间的关系对于理解生命的分子基础至关重要。《Current Topics in Medicinal Chemistry》的目标是促进科学知识和洞察力的增长，推动新治疗剂的发现与开发，以应对人类的重大疾病。对于希望了解最新和最重要进展的药物化学家而言，该杂志是必不可少的。

Category	Quartile
医学	4
医学, 药物化学	4

Applications of Bioorthogonal Chemistry in Tumor-Targeted Drug Discovery

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