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  • SAR Development of Lysine-B...
    Wityak, John; Prime, Michael E; Brookfield, Frederick A; Courtney, Stephen M; Erfan, Sayeh; Johnsen, Siw; Johnson, Peter D; Li, Marie; Marston, Richard W; Reed, Laura; Vaidya, Darshan; Schaertl, Sabine; Pedret-Dunn, Anna; Beconi, Maria; Macdonald, Douglas; Muñoz-Sanjuan, Ignacio; Dominguez, Celia

    ACS medicinal chemistry letters, 12/2012, Letnik: 3, Številka: 12
    Journal Article

    We report a series of irreversible transglutaminase 2 inhibitors starting from a known lysine dipeptide bearing an acrylamide warhead. We established new SARs resulting in compounds demonstrating improved potency and better physical and calculated properties. Transglutaminase selectivity profiling and in vitro ADME properties of selected compounds are also reported.