Peptidomimetics : A New Era in Drug Discovery

Peptides are made up from amino acid sequences which possess importance in various biological processes, making them attractive candidates for therapeutic development. But due to the limitations, such as susceptibility to proteolysis, Blood–brain barrier, poor bioavailability, short half-life, and rapid clearance, suppress their applications in drug development. Peptidomimetics, designed by modification in side chain or the backbone of peptide to mimic the structural and functional properties of peptides to overcome these limitations. After the modification they emerged as a promising class of therapeutic agents in drug discovery and development. Various synthetic strategies such as replacement of natural amino acids with unnatural amino acid, cyclization, implemented to develop peptidomimetics from peptide. Peptidomimetics shows antimicrobial and anticancer properties, also work as immunomodulator. This comprehensive review will help the reader to understand concept of peptidomimetics, their design strategies, diverse applications in various therapeutic areas, limitation and future directions. Graphical Abstract Keywords: Peptidomimetics, Bioavailability, Antimicrobial Activity, Stability