Thiuram Disulfides as Pseudo-irreversible Inhibitors of Lymphoid Tyrosine Phosphatase

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Liste des auteurs: Kulkarni RA, Stanford SM, Vellore NA, Krishnamurthy D, Bliss MR, Baron R, Bottini N, Barrios AM
Editeur: Wiley: 12 months
Année de publication: 2013
Numéro du volume: 8
Numéro de publication: 9
Page d'accueil: 1561
Dernière page: 1568
Nombre de pages: 8
ISSN: 1860-7179
Languages: Anglais-Royaume-Uni (EN-GB)


Résumé

We screened a small library of thiuram disulfides for inhibition of lymphoid tyrosine phosphatase (LYP) activity. The parent thiuram disulfide, disulfiram, inhibited LYP activity in vitro and in Jurkat Tcells, whereas diethyldithiocarbamate failed to inhibit LYP at the concentrations tested. Compound 13, an N-(2-thioxothiazolidin-4-one) analogue, was found to be the most potent LYP inhibitor in this series, with an IC50 value of 3 mu M. Compound 13 inhibits LYP pseudo-irreversibly, as evidenced by the time-dependence of inhibition, with a K-i value of 1.1 mu M and a k(inact) value of 0.004 s(-1). The inhibition of LYP by compound 13 could not be reversed significantly by incubation with glutathione or by prolonged dialysis, but could be partially reversed by incubation with dithiothreitol. Compound 13 also inhibited LYP activity in Jurkat Tcells.


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Dernière mise à jour le 2019-23-08 à 11:15