Recent advances in carbohydrate chemistry and biochemistry afford the opportunity to develop bioactive complex carbohydrates, per se, as drugs or as lead compounds in drug development. Complex carbohydrates are unique among biopolymers in their inherent potential to generate diverse molecular structures. While proteins vary only in the linear sequence of their monomer constituents, individual monosaccharides can combine at any of several sites on each carbohydrate ring, in linear or branched arrays, and with varied stereochemistry at each linkage bond. This chapter addresses some salient features of mammalian glycoconjugate structure and biosynthesis, and presents examples of the biological activities of complex carbohydrates. The chapter presents selected examples that will provide an accurate introduction to their pharmacological potential. In addition to their independent functions, oligosaccharides can modify the activities of proteins to which they are covalently attached. Many glycoprotein enzymes and hormones require glycosylation for expression and function. The chapter discusses the ancillary role of carbohydrates that is of great importance to the use of engineered glycoproteins as pharmaceuticals.
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