Title

Evidence for irreversible inhibition of glycogen synthase kinase-3β by tideglusib.

Journal

The Journal of biological chemistry

Volume

287

Issue

None

Pages

893-904

Date

2012-01-06

Authors

Delgado E | Domínguez JM | Fuertes A | Medina M | Orozco L | del Monte-Millán M

Alsterpaullone showed identical results with the wild-type and the mutant enzymes, demonstrating that its mechanism of inhibition is independent of the presence of the Cys-199 residue.

Inhibition caused by hypothemycin and tideglusib on a panel of selected human recombinant kinases

We report here that tideglusib inhibits GSK-3β irreversibly, as demonstrated by the lack of recovery in enzyme function after the unbound drug has been removed from the reaction medium and the fact that its dissociation rate constant is non-significantly different from zero.

BEL Commons is developed and maintained in an academic capacity by Charles Tapley Hoyt and Daniel Domingo-Fernández at the Fraunhofer SCAI Department of Bioinformatics with support from the IMI project, AETIONOMY. It is built on top of PyBEL, an open source project. Please feel free to contact us here to give us feedback or report any issues. Also, see our Publishing Notes and Data Protection information.

If you find BEL Commons useful in your work, please consider citing: Hoyt, C. T., Domingo-Fernández, D., & Hofmann-Apitius, M. (2018). BEL Commons: an environment for exploration and analysis of networks encoded in Biological Expression Language. Database, 2018(3), 1–11.