Signature of click chemistry in advanced techniques for cancer therapeutics

Abstract

Click chemistry has made a revolution in the field of chemical biology owing to its high efficiency, specificity, and mild reaction conditions. The copper(I)-catalyzed azide–alkyne cycloaddition (CuAAC) and strain-promoted [3 + 2] azide–alkyne cycloaddition (SPAAC) stand out as the most popular click reactions that construct a stable triazole ring by reacting an azide with an alkyne. These two reactions represent an ideal choice for biological applications due to its specificity, reliability, and biocompatibility. As a powerful modular synthetic approach for creating new molecular entities, it has seen increasing use in anticancer drug discovery. The present “state of the art” focuses mainly on the signature of click chemistry (CuAAC and SPAAC) in advanced techniques for cancer therapeutics, which includes cancer immunotherapy, antibody–drug conjugates, development of proteolysis-targeting chimeras, targeted dual-agent combination therapy for cancer, exosome modification for cancer therapy, and photodynamic therapy (PDT).