Biopharmaceutical Discovery by Organic Synthesis

Abstract

Glycoprotein drugs have a remarkable structural complexity among biopharmaceuticals. The main reason for this is the diversity and complexity of their glycans. We have become able to prepare, in high-purity and large quantities, glycans which are extremely difficult to artificially control with posttranslational modification. We have also established a method of adding uniform glycans to arbitrary positions. These technologies make it possible to prepare homogeneous glycoproteins that are extremely difficult to prepare by expression. In addition, because glycans can be introduced to new arbitrary positions, appropriate design of the position, number, and structure of these sugar chains has made it possible to create next-generation biopharmaceuticals.