When Supramolecular Chemistry Meets Chemical Biology: New Strategies to Target Proteins through Host‐Guest Interactions

Abstract Supramolecular chemistry for targeting proteins is of great interest for the development of novel approaches to recognize, isolate and control proteins. Taking advantage of chemical biology approaches, such as genetic‐code expansion and enzyme‐mediated ligation, guest recognition elements can be built into proteins of interest, allowing supramolecular control of protein function and regulation. In this viewpoint article, we will discuss the methods, applications, limitations, and future perspectives of supramolecular chemistry for targeting proteins in a site‐specific manner.