STABILIZED BIOACTIVE PEPTIDES AND METHODS OF IDENTIFICATION, SYNTHESIS AND USE

摘要

An intracellular selection system allows concurrent screening for peptidebioactivity and stability. Randomized recombinant peptides are screened forbioactivity in atightly regulated expression system, preferably derived from the wild-type lacoperon.Bioactive peptides thus identified are inherently protease- and peptidase-resistant. Alsoprovided are bioactive peptides stabilized by a stabilizing group at eitherthe N-terminus, theC-terminus, or both. The stabilizing group can take the form of a small stableprotein, such asthe Rop protein, glutathione sulfotransferase, thioredoxin, maltose bindingprotein, orglutathione reductase, or one or more proline residues.