Protein-protein interaction represents animportant and currently underexploited class of targets for chemotherapeuticintervention. They are a challenging class of targets for traditionalsmall-molecule inhibitors, because the surface areas involved in theinteraction are often large and flat. Cyclic peptides provide a potentialsolution to this problem, as they are capable of recognizing large, flat surfaceareas and are metabolically stable. A high-throughput method has been developedto chemically synthesize, screen, and decode combinatorial cyclic peptidelibraries of 107 diversity (Figure 1). This method has been applied to developpotent inhibitors against Src homology 2 domains, peptidyl-prolyl isomerasePin1, HIV capsid protein, and human prolactin receptor. Some of the cyclicpeptide inhibitors have shown potent anticancer activities.

Inhibition of protein-protein interactions with cyclic peptides

239th National Meeting (2010)

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