Human interferon-β is a naturally N-glycosylated cytokine with immunomodulating bioactivity. The N-glycosylation of IFN-β is reported to affect the pharmacokinetics of this glycoprotein. In 2012, the Sakamoto and Kajihara group reported the chemical synthesis of homogeneous glycoprotein interferon-β 48 (IFN-β).[24] The sequence was divided into three segments 46, 44, 45 (sequence:1-67, 68-88, 89-166) which could be assembled by native chemical ligation (Fig 5: Synthetic strategy of the total synthesis of interferon-β by Sakamoto and coworkers) The biological activity of two glycoforms was compared with commercially available human IFN-β with heterogeneous N-glycan structure. Both antitumor activity assay in vitro and in vivo displayed similar bioactivity between synthetic and commercially available IFN-β. This was the first report to demonstrate that synthetic glycoprotein having homogeneous N-glycan structure showed potent bioactivity in vivo. This result indicated that the synthetic homogeneous glycoprotein can be applied as a powerful tool for biological analysis to investigate structure-function relationship of N-glycans.

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