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Updated: May 4, 2026

Author Spotlight: Developing Acetyl-Click Assay for HAT1 Inhibitor Screening
Published on: January 26, 2024
Use of click-chemistry in the development of peptidomimetic enzyme inhibitors
P Fabbrizzi, G Menchi, A Guarna
1Department of Chemistry "Ugo Schiff" , University of Florence, via della Lastruccia 13, I-50019 Sesto Fiorentino, Florence, Italy. andrea.trabocchi@unifi.it.
Abstract:
Cu(I)-catalyzed Azide-Alkyne Cycloaddition (CuAAC) is often utilized in medicinal chemistry to make the triazole moiety as it acts as a non-classical bioisostere of the peptide bond. This useful technique can also be applied in the fragment-based assembly of molecular libraries for high-throughput screening. This minireview outlines the application of click-chemistry in the synthesis of enzyme inhibitors with the triazole moiety.
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