Kai Waløen, Kunwar Jung-Kc, Elisa D Vecchia, Sunil Pandey, Norbert Gasparik, Anne Døskeland, Sudarshan Patil, Rune Kleppe, Jozef Hritz, William H J Norton, Aurora Martinez, Jan Haavik
The 14-3-3 proteins constitute a family of adaptor proteins with many binding partners and biological functions, and they are considered promising drug targets in cancer and neuropsychiatry. By screening 1280 small-molecule drugs using differential scanning fluorimetry (DSF), we found 15 compounds that decreased the thermal stability of 14-3-3 ζ Among these compounds, ebselen was identified as a covalent, destabilizing ligand of 14-3-3 isoforms ζ , ε , γ , and η Ebselen bonding decreased 14-3-3 ζ binding to its partner Ser19-phosphorylated tyrosine hydroxylase...
August 2021: Molecular Pharmacology