Toward Realization of Bioorthogonal Chemistry in the Clinic

In the last decade, the use of bioorthogonal chemistry toward medical applications has increased tremendously. Besides being useful for the production of pharmaceuticals, the efficient, nontoxic reactions open possibilities for the development of therapies that rely on in vivo chemistry between two bioorthogonal components. Here we discuss the latest developments in bioorthogonal chemistry, with a focus on their use in living organisms, the translation from model systems to humans, and the challenges encountered during preclinical development. We aim to provide the reader a broad presentation of the current state of the art and demonstrate the numerous possibilities that bioorthogonal reactions have for clinical use, now and in the near future.