A Transition State Analogue of 5′-Methylthioadenosine Phosphorylase Induces Apoptosis in Head and Neck Cancers

    Indranil Basu, Grace Cordovano, Ishita Das, Thomas J. Belbin, Chandan Guha, Vern L. Schramm
    The study demonstrated that MT-DADMe-ImmA, a potent inhibitor of MTAP, effectively induced apoptosis in head and neck cancer cell lines FaDu and Cal27 by increasing MTA levels and decreasing polyamines, leading to mitochondrial changes and activation of caspases. This treatment selectively targeted cancer cells without affecting normal fibroblasts, suggesting its potential as a cancer treatment. In a mouse model, MT-DADMe-ImmA led to tumor remission, highlighting its promise for cancers sensitive to DNA methylation changes. Despite inducing apoptosis, the treatment did not alter the protein levels of mitochondrial markers Bcl2 and Bax.
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