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Sialyltransferase Inhibition and Recent Advances
Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics
  • Libo Wang, Harbin Medical University
  • Ying Liu, Harbin Medical University
  • Lijun Wu, Harbin Medical University
  • Xue-Long Sun, Cleveland State University
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Sialic acids, existing as terminal sugars of glycoconjugates, play important roles in various physiological and pathological processes, such as cell–cell adhesion, immune defense, tumor cell metastasis, and inflammation. Sialyltransferases (STs) catalyze the transfer of sialic acid residues to non-reducing oligosaccharide chains of proteins and lipids, using cytidine monophosphate N-acetylneuraminic acid (CMP-Neu5Ac) as the donor. Elevated sialyltransferase activity leads to overexpression of cell surface sialic acids and contributes to many disease developments, such as cancer and inflammation. Therefore, sialyltransferases are considered as potential drug targets for disease treatment. Inhibitors of sialyltransferases thus are of medicinal interest, especially for the cancer therapy. In addition, sialyltransferase inhibitors are useful tool to study sialyltransferase function and related mechanisms. This review highlights recent development of inhibitors of sialyltransferases reported since 2004. The inhibitors are summarized as eight groups: 1) sialic acid analogs, 2) CMP-sialic acid analogs, 3) cytidine analogs, 4) oligosaccharide derivatives, 5) aromatic compounds, 6) flavonoids, 7) lithocholic acid analogs, and 8) others. This article is part of a Special Issue entitled: Physiological Enzymology and Protein Functions.


This work was supported by the American Heart Association Grant-in Aid (14GRANT20290002) and Research fund from the Center for Gene Regulation in Health and Disease (GRHD) at Cleveland State University(GRHD08) supported by Ohio Department of Development (ODOD). L. Wang appreciates the China Oversea Scholar Award from China Scholarship Council.

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Creative Commons Attribution-Noncommercial-No Derivative Works 4.0
Citation Information
Wang, L.; Liu, Y.; Wu, L.; Sun, X. Sialyltransferase inhibition and recent advances. Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics 2016, 1864, 143-153.