生物正交反应在我国的研究进展

Recent Progress of Bioorthogonal Chemistry in China

生物正交反应是指能够在生物体系中进行、且不会与天然生物化学过程相互干扰的一类化学反应.这类反应的出现为科学家对生命进程的原位研究带来了革命性的技术,已经成为化学生物学这一新兴交叉领域的核心方向之一.自这一概念提出的近二十年里,生物正交化学经历了反应类型由单一的“偶联反应”向成键偶联、断键剪切反应并重,应用场景由简单的活细胞体系向更为复杂的生物活体升级的一系列发展历程.同时,在生命科学研究、医药研发、临床诊疗等多个领域展示出了广阔的应用前景.我国化学生物学领域的学者们积极参与并推动了生物正交反应的快速发展,在反应开发、体系优化和实际应用等方面开展了一系列原创工作,取得了瞩目的成绩;尤其是在“生物正交剪切反应”概念的提出与开发应用等方面产生了重要的国际影响.本综述中,分别按照金属介导、光介导和化学小分子介导的生物正交偶联反应以及生物正交剪切反应,对近五年来我国学者在该领域的代表性成果进行系统介绍.最后对生物正交反应的进一步发展与应用加以展望.我们期待更多高效、兼容的生物正交反应得以发展,并提出“遥控生物正交化学”的未来发展目标,期待更多的化学家能够加入生物正交反应的开发拓展与应用探索当中.

Bioorthogonal chemistry refers to chemical reactions that can be carried out in biological systems without inter-fering with natural biochemical processes.During the past two decades since its emergence,the scope of bioorthogonal chemistry has been greatly expanded from ligation to cleavage reactions,with broad applications ranging from live cells to animals for biological studies,medical as well as pharmaceutical research.Chinese chemical biologists have actively partici pated in this exciting area,and a series of important work has been carried out with notable achievements.In particular,the creation and development of bioorthogonal cleavage reactions and its diverse applications have drawn considerable atten tions.In this review,we summarize the representative work on bioorthogonal chemistry that been developed in China in re cent five years.These works will be categorized into metal-,photo-and small molecule-mediated bioorthogonal ligation as well as cleavage reactions,respectively.In the end,we will discuss the future development along this exciting avenue and the further innovation of the“remote-control bioorthogonal chemistry”,which may eventually drive the bioorthogonal reactions into living animals or even human being.