Tideglusib as a First-in-Class Chemical Probe for NatA: Identification, Mechanism, and Cellular Validation of an Allosteric, CoA-Dependent Inhibitor.
Tideglusib is established as a mechanistic chemical probe for NatA, NatA is revealed as a previously unrecognized molecular target for a promiscuous clinical-stage investigational compound, and a conceptual framework for exploiting catalysis-dependent adduct formation as a new strategy for acetyltransferase inhibitor d...