New tools for carbohydrate sulfation analysis: heparan sulfate 2-O-sulfotransferase (HS2ST) is a target for small-molecule protein kinase inhibitors

We report the susceptibility of HS2ST to a variety of cell-permeable compounds in vitro, including polyanionic polar molecules, the protein kinase inhibitor rottlerin and oxindole-based RAF kinase inhibitors. In a related study, published back-to-back with the present study, we demonstrated that tyrosyl protein sulfotranferases are also inhibited by a variety of protein kinase inhibitors. We propose that appropriately validated small-molecule compounds could become new tools for rapid inhibition of glycan (and protein) sulfation in cells, and that protein kinase inhibitors might be repurposed or redesigned for the specific inhibition of HS2ST.

Source: Biochemical Journal - August 14, 2018 Category: Biochemistry Authors: Byrne, D. P., Li, Y., Ramakrishnan, K., Barsukov, I. L., Yates, E. A., Eyers, C. E., Papy-Garcia, D., Chantepie, S., Pagadala, V., Liu, J., Wells, C., Drewry, D. H., Zuercher, W. J., Berry, N. G., Fernig, D. G., Eyers, P. A. Tags: Research Articles Source Type: research