Biocompatible Chemistry: A Plug‐and‐Play Toolbox for Chemical Biology Research

Chemistry is referred to as the central science that has been widely applied in biological, material, and clinical research. Specifically, chemical biology is an interdisciplinary subject, where well‐designed chemical tools and approaches are employed to solve complex biological questions. In the past few decades, the development of biocompatible reactions, which include click chemistry and bioorthogonal chemistry, is one of the most significant advances in the chemical biology field. In short, biocompatible chemistry enables the cleavage and formation of chemical bonds under physiological conditions, which can be thus utilized for specific labeling of cellular biomacromolecules of interest, biomarker/target validation, signaling pathway identification, drug discovery, and so on. The plug‐and‐play nature of biocompatible chemistry makes it a powerful toolbox for investigating complicated biological systems and producing drug leads for clinical usages. In this article, the commonly used biocompatible reactions and the recent advances of their representative applications in chemical biology research is summarized, thus highlighting the diverse potential of biocompatible chemistry as a plug‐and‐play toolbox for future basic and translational studies.