Sharpless-Bertozzi-Meldal click Chemistry

Three scientists win Nobel Prize for ‘click Chemistry’

Image credit: Johan Jarnestad/The Royal Swedish Academy of Sciences

The trio developed ‘click Chemistry’, an environmentally-friendly method for rapidly joining molecules to develop cancer treatments, create materials and illuminate the workings of cells.

Professor Carolyn R Bertozzi from Stanford University, Professor Morten Meldal from the University of Copenhagen, and Professor K Barry Sharpless from Scripps Research, have received the coveted Nobel Prize "for the development of click Chemistry and bioorthogonal chemistry”.

The three will share the 10 million Swedish krona (£800,000) award. 

The work reportedly "transformed" how chemistry can be done, making it simpler and more effective, by allowing molecules to link together, like Lego pieces. Moreover, their work can also ensure that many reactions can be done with minimum impact on the environment. 

This would be the second Nobel Prize awarded to Sharpless, who received this award for the first time in 2001 for chiral catalysts. Bertozzi, who pioneered bioorthogonal chemistry that links living cells, is the eighth woman to win the Chemistry Nobel.

"I'm absolutely stunned. I can hardly breathe," she said. 

Morten Meldal, from Denmark, told BBC News he was "shaking for half an hour" after he found out he won.

Building new molecules is a complex process that often requires a multitude of sequential individual reactions, each one hampered by side reactions that reduce the purity of the sample. This increases the number and complexity of any further reaction steps, while producing harmful waste that needs careful and expensive disposal.

The concept of ‘click Chemistry’ was developed by Sharpless at the turn of the millennium. It’s a process by which molecules are simply, quickly, reliably and repeatedly joined together, similar to a Lego set. He stipulated that click reactions should be carried out in water, instead of harmful solvents commonly used by synthetic chemists to dissolve their reactants. 

Bertozzi's groundbreaking discovery made click Chemistry work in living cells, meaning scientists could do "chemistry inside the human body, to make sure drugs go to the right place and stay away from the wrong place", she said.

To achieve this, she attached the azide ‘buckle’ to a sugar molecule. This gets absorbed to the cell, incorporated, and presented on the cell’s surface. A modified alkalyne (the clip) connected to a green fluorescent molecule then gets added to the cell where it clicks to the azide sugar. Then the cell can be easily tracked under a microscope.

This technique has led to insights into the behaviour of tumour cells. It has also helped to target radiotherapies directly to cancer cells, reducing the harm to nearby healthy cells, and applications in pharmaceuticals, DNA sequencing and materials with added functionality (such as magnetic and electrical).  

It is a "biological discovery tool" that allows scientists to see new molecules that we didn't know existed, Bertozzi explained.

The Nobel committee praised the scientists' work for making chemistry functional and said they had an enormous impact on science.

"This year's prize deals with not overcomplicating matters, instead working with what is easy and simple," said Johan Åqvist, chair of the Nobel Committee for Chemistry.

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