Structure–activity relationship of biological macromolecules

Biological macromolecules are naturally occurring large cellular components responsible for a wide array of functions necessary for the growth and survival of living organisms. They also possess various bioactivities such as antimicrobial, antioxidant, antitumor, antiviral, antiinflammatory, antiproliferative, and hypoglycemic activities. The growing interest in bioactive macromolecules as potential therapeutical drugs has driven scientists to further study the association between their chemical structures and corresponding functions/activities. This chapter aims to provide a short overview on the structural features influencing the bioactivities of several biological macromolecules, namely l -amino acid oxidases, lysostaphin and metallo-β-lactamase-like lactonase and chitosan. As observed in this chapter, establishing the structure–activity relationship (SAR) can often prove to be challenging for macromolecules given the complexity of the three-dimensional organization level of proteins and the branched chains of the carbohydrates. Nevertheless, certain structural features influencing the bioactivities of macromolecules have been identified and could help to accelerate their development and application in the biomedical field. Indeed, a comprehensive understanding of biomacromolecule SARs remains necessary as information inferred from these studies may be crucial to many aspects of drug discovery and development, whether it is for primary screening or lead optimization, as well as for the designing of synthetic derivatives with improved properties.