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

ABSTRACT: There is a great demand for the discovery of new therapeutic molecules that combine the high specificity and affinity of biologic drugs with the bioavailability and lower cost of small molecules. Small, natural-product-like peptides hold great promise in bridging this gap; however, access to libraries of these compounds has been a limitation. Since ribosomal peptides may be subjected to in vitro selection techniques, the generation of extremely large libraries (>10(13)) of highly modified macrocyclic peptides may provide a powerful alternative for the generation and selection of new useful bioactive molecules. Moreover, the incorporation of many non-proteinogenic amino acids into ribosomal peptides in conjunction with macrocyclization should enhance the drug-like features of these librarie

SUBMITTER: Schlippe YV 

PROVIDER: S-EPMC3384292 | biostudies-literature | 2012 Jun

REPOSITORIES: biostudies-literature