Abstract

Bioorganic chemistry, an interdisciplinary scientific branch of chemistry and biology, has grabbed considerable impetus in the last few decades, owing to its important insights into the functioning of biological systems at the molecular level. Primarily it is a discipline of science that involves the study of biological processes mainly proteins and peptides at transcriptional, translational, or posttranslational levels. Yet, at the molecular level, our basic knowledge and understanding of the structureactivity relationship (SAR) of peptides/proteins remain in their infancy. Indeed, the dissection of multidomain proteins into small and simpler fragments, shed light on the design of scaffolds that seems to mimic the function of natural proteins in an efficient way, thereby giving rise to the birth of PEPTIDOMIMETICS. At times, the mimetics of critical functional protein domains, are advantageous over normal proteins/peptides in terms of specificity and therapeutic benefits. Henceforth the latter are considered to be expensive models for the investigation of molecular recognition. In this book chapter, our effort lies in modulating the basics of principles of peptide chemistry, challenges encountered, and some very efficient examples of how Peptidomimetics serves as a road map to resolve various stumbling blocks for PROTEOLYSIS and others.