Drugs affecting glycosaminoglycan metabolism

• A classification of drugs affecting glycosaminoglycan (GAG) metabolism is provided.
• Rationally designed small molecule drugs display in vivo efficacy.
• A number of clinically approved drugs affect GAG metabolism.
• Strategies are proposed for the discovery of drugs specifically affecting GAGs.

Glycosaminoglycans (GAGs) are charged polysaccharides ubiquitously present at the cell surface and in the extracellular matrix. GAGs are crucial for cellular homeostasis, and their metabolism is altered during pathological processes. However, little consideration has been given to the regulation of the GAG milieu through pharmacological interventions. In this review, we provide a classification of small molecules affecting GAG metabolism based on their mechanism of action. Furthermore, we present evidence to show that clinically approved drugs affect GAG metabolism and that this could contribute to their therapeutic benefit.