Introduction: Among protein and fibers in the extracellular matrix (ECM), collagen is the most copious and widely employed in cosmetic, food, pharmaceutical, and biomedical industries due to its extensive biocompatible and versatile properties. In the last years, the knowledge about functions of collagens increased and expanded dramatically. Once considered only crucial for the ECM scaffolding and mechanotransduction, additional functional roles have now been ascribed to the collagen superfamily which are defined by other recently discovered domains, supramolecular assembly and receptors.Areas covered: Given the importance of each step in the collagen biosynthesis, folding and signaling, medicinal chemists have explored small molecules, peptides, and monoclonal antibodies to modulate enzymes, receptors and interactions with the physiological ligands of collagen. These compounds were also explored toward diseases and pathological conditions. The authors discuss this providing their expert perspectives on the subject area.Expert opinion: Understanding collagen protein properties and its interactome is beneficial for therapeutic drug design. Nevertheless, compounds targeting collagen-based interactome suffered from the presence of different isoforms for each target and the lack of specific 3D crystal structures able to guide properly drug design.
Keywords: Collagen; collagen prolyl-4-hydroxylase; discoidin; drug design; drug target; integrin; interactions; metalloproteinase.