自然杂志 ›› 2026, Vol. 48 ›› Issue (2): 122-128.doi: 10.3969/j.issn.0253-9608.2026.02.006

• 专题综述 • 上一篇    下一篇

从分子到生命:点击化学与生物正交化学点亮生物医学未来

金彦佳,陈雪瑞,肖俊杰   

  1. ①上海大学 生命科学学院,上海 200444;②上海大学 医学院,上海 200444
  • 收稿日期:2026-02-01 出版日期:2026-04-25 发布日期:2026-04-20
  • 作者简介:陈雪瑞,研究方向:器官修复的生物材料。 肖俊杰,研究方向:心力衰竭的综合干预和风险预警策略。

From molecules to life: click chemistry and bioorthogonal chemistry illuminate future of biomedicine#br#

JIN Yanjia, CHEN Xuerui, XIAO Junjie   

  1. ① School of Life Sciences, Shanghai University, Shanghai 200444, China; ② School of Medicine, Shanghai University, Shanghai 200444, China
  • Received:2026-02-01 Online:2026-04-25 Published:2026-04-20

摘要: 卡罗琳•贝尔托西(Carolyn R. Bertozzi)、莫滕•梅尔达尔(Morten Meldal)、巴里•沙普利斯(K. Barry Sharpless)因在点击化学和生物正交化学方面的杰出工作获得2022年诺贝尔化学奖。点击化学涉及快速且不可逆地结合两个分子的反应,其中一些反应可以在活细胞内进行,却不影响体内正常的生化过程。这实现了人体中化学分子的“精准合成”,使得“活体合成药物”“体内3D打印组织”从概念走向临床。因此,始于有机合成的点击化学在细胞和癌症治疗中得到广泛的应用。本文具体介绍了点击化学与生物正交化学在精准成像、靶向治疗、基因工程和病毒疫苗等领域的应用。随着反应体系的不断优化和新反应的开发,它们将不断推动个性化医疗、新药研发、再生医学的发展。

关键词: 点击化学, 生物正交化学, 生物材料, 生物医学

Abstract: Carolyn R. Bertozzi, Morten Meldal, and K. Barry Sharpless received the 2022 Nobel Prize in Chemistry, attributed to their study on click chemistry and bioorthogonal chemistry. Click chemistry aims to rapidly and reliably synthesize various molecules by linking small units, while bioorthogonal reactions apply this to specially label and visualize living systems without interfering the biological surrounding. “Precise synthesis” has been introduced into the human body, enabling the clinical translation of “drug synthesis in vivo” and “3D bioprinting of tissues in vivo”. Therefore, click chemistry that started with organic chemistry have been widely applied in cancer therapy. The applications of click chemistry and bioorthogonal chemistry in precise imaging, targeted therapy, genetic engineering, and viral vaccines are summarized in this work. The practical application of personalized medicine, new drug research and development, and regenerative medicine are constantly promoted.