4 Applications of Click Chemistry

This year’s Nobel Prize in Chemistry didn’t spotlight complex scientific methods or breakthroughs like Helium Microscopy. Instead, it recognised a framework founded in function and simplicity. Developed by American chemist K. Barry Sharpless and Danish chemist Morten Meldal, click chemistry takes a minimalist approach to molecular synthesis.

The click chemistry toolbox includes a series of high-yield, modular reactions. These can be used to ‘snap’ together molecular building blocks and assemble more complex organic molecules. Thanks to fellow Nobel laureate Carolyn Bertozzi who developed copper-free bioorthogonal reactions, click chemistry can also be used in living organisms.

Below, we explore four key applications for click chemistry:

1. DNA labelling

Click chemistry has revolutionised DNA labelling and made it possible to use several fluorescent dyes that were previously unsuitable. These include red coumarin azide and blue phenoxazinium azide. DNA labelling is widely used in molecular biology labs and allows scientists to observe how proteins interact with nucleotides on a molecular level.

2. Drug discovery

Molecular synthesis is at the heart of drug discovery and click chemistry makes the process faster, easier and simpler than ever. In an article published in the journal Cancer Biotherapy and Radiopharmaceuticals, the authors explore how click chemistry was used to develop new treatments for Type II diabetes. Research published in the German journal Angewandte Chemie introduces how click chemistry can be used to inhibit HIV-1-PR, an enzyme that supports the HIV virus and promotes the onset of AIDS.

3. Materials science

Click chemistry is compatible with various functional groups, making it ideal for the materials science sector. Scientists use the technique to understand the unique properties of materials and develop new products. In an article published in the journal Biomaterials Science & Engineering, the authors describe how click chemistry is used to design hydrogels for tissue engineering and regenerative medicine applications.

4. Radiochemistry

Radiochemistry is another field that’s been transformed by the introduction of click chemistry. The discipline focusses on the chemistry of radioactive materials, with imaging techniques like positron emission tomography (PET) and single photon emission computed tomography (SPECT) used for analysis.

An article published in the peer-reviewed journal Bioconjugate Chemistry lists the four main advantages click chemistry has provided to the radiochemistry field. These include:

• The development of prosthetic groups for radiolabeling reactions
• Easy radiolabeling of peptides and proteins
• The ability to build and customise scaffolds for radiometals
• The development of highly effective in vivo pre-targeting methods

This article just scratches the surface of click chemistry. Find out more about the Nobel Prize-winning framework in our complete guide, ‘What is Click Chemistry? Everything You Need to Know’.