Physical Sciences and Mathematics Commons^™

Side Chain Modifications To Improve Peptide Structure–Activity Relations, Neelam Lahankar

Seton Hall University Dissertations and Theses (ETDs)

While natural peptides, are ideal starting points for peptide-based drug design and development, they suffer from high conformational instability, which results in susceptibility to proteolytic degradation and poor bioavailability. Peptidomimetics in recent years has helped circumvent these shortcomings by improving the pharmacological properties of polypeptides. Peptidomimetics contain essential elements (pharmacophores) that mimic a natural peptide or protein in 3D space and retain the ability to interact with the biological target producing the same biological effect. In contrast, they offer conformationally restricted structures, potentially minimizing cross-target interactions, which leads to better transport properties through biologic membranes and resistance to immune responses. …