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.
Keywords: Amino acids, Helix, Ramachandran map, Sheets, Turns.
