Download MendeleyThe Inhibition of Polysialyltranseferase ST8SiaIV Through Heparin Binding to Polysialyltransferase Domain (PSTD).
Peng, L.X., Liu, X.H., Lu, B., Liao, S.M., Zhou, F., Huang, J.M., Chen, D., Troy II, F.A., Zhou, G.P., Huang, R.B.(2019) Med Chem 15: 486-495
- PubMed: 30569872
- DOI: https://doi.org/10.2174/1573406415666181218101623
- Primary Citation of Related Structures:
6AHZ - PubMed Abstract:
The polysialic acid (polySia) is a unique carbohydrate polymer produced on the surface Of Neuronal Cell Adhesion Molecule (NCAM) in a number of cancer cells, and strongly correlates with the migration and invasion of tumor cells and with aggressive, metastatic disease and poor clinical prognosis in the clinic. Its synthesis is catalyzed by two polysialyltransferases (polySTs), ST8SiaIV (PST) and ST8SiaII (STX). Selective inhibition of polySTs, therefore, presents a therapeutic opportunity to inhibit tumor invasion and metastasis due to NCAM polysialylation. Heparin has been found to be effective in inhibiting the ST8Sia IV activity, but no clear molecular rationale. It has been found that polysialyltransferase domain (PSTD) in polyST plays a significant role in influencing polyST activity, and thus it is critical for NCAM polysialylation based on the previous studies.
Organizational Affiliation:
Life Science and Technology College, Guangxi University, Nanning, Guangxi, 530004 China; 2Institute of Biophysics, Chinese Academy of Sciences, Beijing, China.
