Peptidomimetics in Drug Discovery: Challenges, Strategies and Therapeutic Application

Peptidomimetics plays a crucial role in drug development by mimicking endogenous peptides and overcoming obstacles such as instability, fast metabolism, and elimination. These compounds have been developed since the 1950s using approaches such as cyclization and the addition of non-natural amino acids, which improve their stability and effectiveness in treatment. Peptidomimetics, which are categorized according to their structural and functional features, have a wide range of uses, such as hormonal replacement therapy and antibacterial, antidiabetic, anticancer, and analgesic properties. This chapter focuses on the limitations of peptide delivery, challenges associated with peptidomimetics designing, computational approaches employed, classification, synthetic approach, and therapeutic applications of peptidomimetics. It emphasizes their ability to enhance the stability and effectiveness of drugs, as well as their therapeutic potential.