Site-Specific Introduction of Sialic Acid into Insulin

摘要

Insulin, a peptide hormone, is virtually the only effective drug for the treatment of diabetes.111 The quantity of insulin required is increasing along with the number of patients, and the demand for insulin can be as much as 0.5-1.0 g per year per patient. However, native insulin is broken down in the blood stream within a few hours of administration, mainly as a result of decomposition in the liver. Several insulin derivatives have been investigated as possible long-acting insulins for decreasing the required frequency of administration. Most of these insulin derivatives are less soluble than native insulin and are gradually released from the injection site into the blood stream. The disadvantages of these long-acting insulins are in the complex administration procedure and the difficulty in controlling the circulating glucose levels. It is expected that water-soluble long-acting insulin derivatives would overcome these problems.