Unique and specific ligands to target proteins play an important role in academic research, clinical diagnostics and drug discovery. Currently, small molecules, peptides or even antibodies have been investigated as novel ligands to disease-related proteins. However, the diversity limit of small molecules and the low stability of peptides and antibodies have hindered the identification of suitable drug candidates for some disease targets.
Peptoids, oligomers of N-substituted glycines, were developed as peptide mimetics for the generation of chemically diverse libraries of novel molecules . The chemical structure of a peptoid shifts the side chain of peptides from α-carbon to nitrogen (See above). From highly diverse peptoid libraries, unique peptoid ligands have been identified to several disease-related targets, including the β4 proteasome subunit, VEGF receptor 2, Huntingtin polyQ expansion. [2, 3, 4].
For more information on peptoid synthesis, peptoid libraries and applications, click here.