AAT Bioquest

What are the most common pharmaceutical applications of click chemistry?

Posted April 10, 2024


Some common pharmaceutical applications of click chemistry include: drug discovery, polymer chemistry, drug delivery, and bioconjugation

  • In drug discovery, click chemistry is used to synthesize libraries of compounds for future drug use. Click chemistry offers a straightforward approach to creating 1,2,3-triazoles, which exhibit excellent pharmacological properties. These compounds have been extensively used in the synthesis of various antiviral, anticancer, and antibacterial drugs. 
  • In bioconjugation, click chemistry enables the conjugation of drugs or targeting ligands to biomolecules such as peptides or proteins. This facilitates applications such as cell-surface labeling as well as DNA modification and labeling. 
  • Click chemistry plays a significant role in drug delivery by facilitating the design and synthesis of drug delivery systems. For example, in the development of nanoparticles, click chemistry is commonly utilized to attach antibodies to the nanoparticle surface. Antibodies exhibit the ability to enhance binding to specific cell lines. Since antibodies are large proteins with critical binding sites, it is essential to ensure that click chemistry does not interfere with these binding sites during attachment to the nanoparticle surface. 
  • Click chemistry is also involved in five types of polymer synthesis which includes: block copolymer synthesis, dendrimer synthesis, polymer network synthesis, polymer analogous modification, and linear multifunctional copolymer synthesis. Click chemistry enhances product yields and also simplifies purification processes and synthetic procedures in these applications. 
Additional resources

Growing Applications of “Click Chemistry” for Bioconjugation in Contemporary Biomedical Research

Click Chemistry

FastClick™ Cy3 Azide