To identify molecular ligands that recognize peptides or proteins is a fundamental challenge in drug discovery research. Here, we report a novel One-Bead-Two-Compound (OBOC) combinatorial library which based on the macrocyclic peptidomimetics-γ-AApeptides. In this strategy, the coding tag was synthesized by applying the Dde-protected α-amino acids, which were confirmed to have good compatibility with the synthesis of γ-AApeptides on the solid phase. The library was screened against the receptor tyrosine kinase EphA2 and one compound was discovered have good binding with the protein. This new macrocyclic library strategy may provide a new source of ligands for the discovery of the molecular probes or therapeutic agents.<br/>

High-throughput cyclic γ-AAPeptides screening library against EPHA2

254th National Meeting (2017)

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