In vitro selection of highly modified cyclic peptides that act as tight binding inhibitors.

摘要: There is a great demand for the discovery of new therapeutic molecules that combine high specificity and affinity biologic drugs with bioavailability lower cost small molecules. Small, natural-product-like peptides hold promise in bridging this gap; however, access to libraries these compounds has been limitation. Since ribosomal may be subjected vitro selection techniques, generation extremely large (>1013) highly modified macrocyclic provide powerful alternative useful bioactive Moreover, incorporation many non-proteinogenic amino acids into conjunction macrocyclization should enhance drug-like features libraries. Here we show mRNA-display, technique allows peptides, can applied evolution contain majority unnatural acids. We describe isola...