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“Click chemistry” developers awarded Nobel Prize

“Click chemistry and bioorthogonal reactions have taken chemistry into the era of functionalism,” the jury explained

Caroline R. Bertozzi and Barry Sharpless of the United States have been awarded the 2022 Chemistry Nobel Prize together with Denmark's Morten Meldal for making difficult things easy, it was announced.

The winners were chosen “for the development of click chemistry and bioorthogonal chemistry,” the organizers explained in a more technical manner. Bertozzi is based at Stanford University in California, Sharpless with Scripps Research, California, and Meldal is at the University of Copenhagen, Denmark

Sharpless and Meldal have laid the groundwork for a functional form of chemistry in which molecular building blocks come together quickly and efficiently, while Bertozzi has taken click chemistry to a new dimension and has begun to use it in living organisms.

“This year's Chemistry Prize is about not overcomplicating things, but working with what is easy and simple,” explained Johan Åqvist, Chairman of the Nobel Committee for Chemistry. “Functional molecules can be built even by following a simple path.” Click chemistry has applications in the field of medical science, including the treatment of cancer.

Sharpless became the fifth person to win a Nobel for the second time. It was Sharpless who in 2000 coined the concept of click chemistry, which the Nobel Committee for Chemistry defines as a simple, straightforward, and reliable form of chemistry in which reactions are fast and unwanted by-products are avoided.

Shortly thereafter Meldal and Sharpless independently presented what is now the crown jewel of click chemistry, a chemical reaction that is widely used for developing pharmaceuticals, mapping DNA, and creating materials.

The Nobel Committee underlined that Bertozzi took click chemistry to a new level by applying it to living organisms. “Thanks to bioorthogonal reactions, researchers have improved the targeting of cancer drugs, which are now being tested in clinical trials,” the Nobel Committee noted. “Click chemistry and bioorthogonal reactions have brought chemistry into the era of functionalism. This is bringing the greatest benefits to mankind.”

Bertozzi, using the work of Sharpless and Meldal, came up with an efficient and innovative method to map glycans, which are carbohydrate-based polymers made by all living organisms. According to the Nobel website, “One area that Bertozzi focuses on is glycans on the surface of tumor cells. Her studies have led to the insight that some glycans appear to protect tumors from the body’s immune system, as they make the immune cells shut down. To block this protective mechanism, Bertozzi and her colleagues have created a new type of biological pharmaceutical. They have joined a glycan-specific antibody to enzymes that break down the glycans on the surface of the tumor cells. This pharmaceutical is now being tested in clinical trials on people with advanced cancer.”

According to the Nobel website, “Instead of trying to wrangle reluctant carbon atoms into reacting with each other, Barry Sharpless encouraged his colleagues to start with smaller molecules that already had a complete carbon frame. If chemists choose simple reactions – where there is a strong intrinsic drive for the molecules to bond together – they avoid many of the side reactions, with a minimal loss of material. Sharpless called this robust method for building molecules click chemistry, saying that even if click chemistry cannot provide exact copies of natural molecules, it will be possible to find molecules that fulfill the same functions.”

Sharpless came up with the term 'click chemistry' and worked extensively on it, Meldal, independently of Sharpless, came up with a special chemical structure called 'triazole' which has many significant applications, and Bertozzi took the next step of developing click reactions that could work inside living organisms -- 'bioorthogonal' reactions (a term she coined), take place living systems without interfering with native biochemical processes.

Chemists often try to recreate complex chemical molecules found in nature, and this has applications, among other things, in the field of medicine – how to target and block pathogens in cells. However, this process can be complicated and time-consuming.

The announcements will continue Thursday with the Literature Prize, Friday with the Peace Prize, and Monday with the Economics Prize.