Research paperEpidermal growth factor receptor signaling cascade as target for tyrphostin (RG 50864) in epithelial cells: Paradoxical effects on mitogen-activated protein kinase kinase and mitogen-activated protein kinase activities☆
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2008, Chemistry and BiologyCitation Excerpt :Two chemicals designed to target either tyrosine kinases (tyrphostin 47) or tyrosine phosphatases (NSC95397 and Me-3,4-dephostatin) were also found to inhibit TGM2 but did so less potently than ZM39923, which was designed to target Janus kinase 3, suggesting that TGM2 shares a similar kinase-like binding site (Faaland et al., 1991; Liu, 2003; Peyregne et al., 2005; Prevost et al., 2003; Suzuki et al., 2001; Tamura et al., 2000; Wolbring et al., 1994). Tyrphostin compounds target tyrosine kinases by binding to the kinase substrate binding site (Nowak et al., 1997). The tyrosine kinase inhibitors used to inhibit TGM2 are used at ∼100 μM in most cellular studies (Bain et al., 2003; Davies et al., 2000); however, our findings suggest Ca-TGM2 is a target at lower concentrations.
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This work was supported by the Association pour la Recherche sur le Cancer (grant 3014), by Institut National de la Santé et de la recherche Médicale (INSERM), Centre National de la Recherche Scientifique (CNRS) and by the Institut de la Formation Supérieure Biomédicale (IFSBM).