ARTICLES

Studies toward Chemical Synthesis of Homogeneously Glycosylated Interleukin-10

  • Weidong Dong ,
  • Haiyun Liu ,
  • Xinyu Li ,
  • Biao Wang ,
  • Bo Cheng ,
  • Suwei Dong
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  • State Key Laboratory of Natural and Biomimetic Drugs, Chemical Biology Center, and Department of Chemical Biology at School of Pharmaceutical Sciences, Peking University, Beijing 100191
(These authors contributed equally to this work).

Received date: 2024-10-02

  Revised date: 2024-11-07

  Online published: 2024-12-20

Supported by

National Natural Science Foundation of China(92153301); National Natural Science Foundation of China(22321005)

Abstract

Human cytokine interleukin-10 (IL-10) sequence contains a conserved N-glycosylation sequon, Asn-Lys-Ser, but the presence and functional significance of this glycosylation have not been previously studied. Here, the chemical synthesis and characterization of IL-10 and its glycosylated form were explored. Using solid-phase peptide synthesis, native chemical ligation, and metal-free desulfurization, the full-length IL-10 was assembled and the non-glycosylated protein was successfully obtained through optimizing the refolding conditions. Building on this synthetic route, an N-acetylglucosamine (N-GlcNAc) modification was introduced into the peptide segment via cassette strategy, and further elaborated into Asn116 N-mono- saccharide-modified IL-10. Mass spectrometry (MS) and circular dichroism analysis of the synthesized IL-10 variants have suggested that they have similar structures to that of the biologically expressed counterpart.

Cite this article

Weidong Dong , Haiyun Liu , Xinyu Li , Biao Wang , Bo Cheng , Suwei Dong . Studies toward Chemical Synthesis of Homogeneously Glycosylated Interleukin-10[J]. Chinese Journal of Organic Chemistry, 2025 , 45(3) : 951 -958 . DOI: 10.6023/cjoc202410001

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