The bioorthogonal revolution

Bioorthogonal chemistry

Source: © Melvin Galapon @ Début Art

A set of reactions operating silently inside live cells or whole animals are lighting up chemical biology and inspiring new medicines, James Mitchell Crow finds

Few pieces of research transition from idea to reality quite so swiftly as a particular project from Carolyn Bertozzi’s labv in the early 2000s. But sometimes, things just click. The team was looking for new reactions that could be used to selectively tag target biomolecules inside living cells, when Bertozzi struck upon the idea of using strained substrates to drive reactivity. Today, that concept has carried all the way to human use. Strain-driven bioorthogonal chemistry is now being tested in a first-in-human clinical trial of an experimental anticancer therapeutic that selectively releases the drug at the tumour site.