Carolyn Bertozzi, Morten Meldal and Barry Sharpless share Nobel Prize in Chemistry

The Royal Swedish Academy of Sciences has decided to award the 2022 Nobel Prize in Chemistry to Carolyn R Bertozzi from Stanford University, California, USA; Morten Meldal of the University of Copenhagen, Denmark and K Barry Sharpless of Scripps Research, La Jolla, CA, USA “for the development of click chemistry and bioorthogonal chemistry”.

“It just says it’s a click – and the molecules are coupled together – the 2022 Nobel Prize in Chemistry aims to facilitate difficult processes. Barry Sharpless and Morten Meldal laid the foundations for a functional form of chemistry – chemistry of the click – in which the molecular building blocks fit together quickly and efficiently. Carolyn Bertozzi took the chemistry of the click to a new dimension and began to use it in living organisms,” states a citation from the Nobel Prize Committee .

Chemists have long been driven by the desire to build ever more complicated molecules. In pharmaceutical research, this has often consisted of artificially recreating natural molecules with medicinal properties. This has led to many admirable molecular constructs, but these are usually time-consuming and very expensive to produce, the committee noted.

“This year’s Chemistry Prize is about not over-complicating things, but rather about working with what is easy and simple. Functional molecules can be built even by taking a simple route,” says Johan Aqvist, chairman of the Nobel Committee for Chemistry.

Barry Sharpless – now receiving his second Nobel Prize in Chemistry – got the ball rolling. Around the year 2000, he invented the concept of click chemistry, which is a simple and reliable form of chemistry, where reactions occur quickly and unwanted by-products are avoided.

Soon after, Morten Meldal and Barry Sharpless – independently of each other – presented what is today the crown jewel of click chemistry: the copper-catalyzed azide-alkyne cycloaddition. This is an elegant and efficient chemical reaction that is now widely used. Among many other uses, it is used in the development of pharmaceuticals, to map DNA, and to create materials that are more fit for purpose.

Carolyn Bertozzi has taken click chemistry to a new level. To map important but elusive biomolecules on the surface of cells – glycans – she developed click reactions that work inside living organisms. Its bioorthogonal reactions proceed without disturbing the normal chemistry of the cell.

These reactions are now used globally to explore cells and track biological processes. By using bioorthogonal reactions, researchers have improved the targeting of anti-cancer pharmaceuticals, which are currently being tested in clinical trials.

Click chemistry and bioorthogonal reactions propelled chemistry into the era of functionalism. This brings the greatest benefit to humanity, the committee says.