Peptidomimetics Based Therapy Across Cancer, Diabetes, Infection, Neurological and Cardiovascular Disease

Abstract

Peptidomimetics are synthetic compounds designed to mimic the structural and functional features of natural peptides while overcoming limitations such as poor stability, low bioavailability, and rapid degradation. These compounds maintain the ability to interact with biological targets, offering enhanced receptor selectivity, potency, and pharmacokinetic properties. Traditional classification divides peptidomimetics into structural, functional, and functional-structural types, while modern approaches categorize them into Classes A–D based on similarity to the native peptide. Advanced synthesis methods—including solid-phase peptide synthesis (SPPS), liquid-phase peptide synthesis (LPPS), and hybrid approaches—enable production of complex molecules with improved yields and purity. Local modifications, such as amide bond surrogates, N-methylation, or incorporation of non-natural amino acids, and global restrictions, like cyclization, further optimize stability and bioactivity. Peptidomimetics play a critical role in treating diverse conditions including cancer, type 2 diabetes mellitus, and cardiovascular diseases by modulating key biological pathways. Mechanistically, they influence protein-protein interactions, receptor signaling, and enzymatic activity, with clinical applications expanding rapidly. Market potential continues to grow, driven by technological advancements and demand for targeted therapeutics. This review highlights classification frameworks, design strategies, and synthetic approaches, emphasizing their impact on modern drug discovery and therapeutic development.