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[25 Aug 2011 | No Comment | 4,119 views]
SRC inhibition induces apoptosis through p27 nuclear stabilization

In this short communication, the authors focus on the SRC pathway, which is hyperactivated in MM specimens and cell lines compared with normal mesothelial cells (Menges et al., 2010). Inhibition of the SRC pathway with the multi-targeted inhibitor dasatinib has been shown to result in apoptosis, cell cycle arrest and decreased migration and invasion in mesothelioma cell lines (Tsao et al., 2007).
Here the authors test a panel of newly synthesized pyrazolo[3,4-d]pyrimidine derivative SRC kinase inhibitors, that bind the ATP pocket of the SRC kinase, which effectively inhibit SRC activity at nanomolar concentrations.