Click the images to explore the mechanism and alkyne moiety
Click chemistry is a powerful tool in chemical and biological research, with the Cu(I)-catalysed azide-alkyne cycloaddition (CuAAC) reaction being one of the most efficient and versatile reactions, offering high yields and minimal side reactions.
In 2022, C. Bertozzi, M. Meldal, and K.B. Sharpless were awarded the Nobel Prize in Chemistry for their groundbreaking work on click chemistry and bio-orthogonal chemistry. They demonstrated how bio-orthogonal ligation enables chemical reactions to occur selectively in biological systems without interfering with natural processes. A key concept in this field is orthogonality, where specific functional groups can be modified or removed independently, even in complex environments. This technique is crucial in developing enzyme inhibitors, receptor ligands, and anticancer drugs.
For further details, explore the pages on hydroxyethylamine and benzophenone probes (purple), as this project examines the effect of photo-reactive groups and alkyne integration. They explore how both scaffolds are functionalised with terminal alkynes (orange) which behave as chemical tags, remaining inert until activation. This ensures precise targeting and minimal interference. After photo-crosslinking, the alkyne reacts via a CuAAC reaction, enabling the study of protein-protein and protein-ligand interactions with high specificity, using techniques like fluorescence imaging and mass spectrometry.