Fucanomics and galactanomics: current status in drug discovery, mechanisms of action and role of the well-defined structures

Abstract

Background: With the recent advent of glycomics, many medically relevant glycans have been discovered. Sulfated fucans (SFs) and sulfated galactans (SGs) are one of these classes of glycans with increasing interest to both glycomics and medicine. Besides having very unique structures, some of these molecules exhibit a broad range of pharmacological actions. In certain cases, high levels of effectiveness may be reached when the proper structural requirements are found.

Scope of review: Here, we cover the fundamental biochemical mechanisms of some of these medicinal properties. We particularly focus on the beneficial activities of SFs and SGs in inflammation, hemostasis, vascular biology, and cancer.

Major conclusions: In these clinical systems, intermolecular complexes directly driven by electrostatic interactions of SFs and SGs with P- and L-selectins, chemokines, antithrombin, heparin cofactor II, thrombin, factor Xa, bFGF, and VEGF, overall govern the resultant therapeutic effects. In spite of that, the structural features of SFs and SGs have shown to be essential determinants for formation and stability of those molecular complexes, which consequently account to the differential levels of the biomedical responses.

General significance: Accurate structure-function relationships have mostly been achieved when SFs and SGs of well-defined structures are used for study. Therefore, these types of glycans have become of great usefulness to identify the chemical requirements needed to achieve satisfactory clinical responses.