Abstract

Glycosaminoglycans (GAGs) interact with a large number of human proteins and modulate a number of responses such as growth and differentiation, infection and immune response, etc. One GAG that is routinely utilized in the clinic is heparin. Agents derived from the use of heparin include enoxaparin, dalteparin, tinzaparin and fondaparinux. Other natural GAG agents of special interest include chondroitin sulfate (arthritis) and dermatan sulfate (anticoagulation). Although it has been recognized that many GAG-based agents should reach the clinic, the number of such GAG-based drugs has not increased since the start of millennium. A key reason for this state is that the technology to prepare homogeneous GAG preparations is not available. We have developed a simple enzyme immobilization technology that can help prepare GAG oligosaccharides with high homogeneity. The technology can be applied to prepare oligosaccharides belonging to the heparin-, heparan sulfate-, chondroitin sulfate-, keratan sulfate- or hyaluronic acid- class of GAGs.