Author/Authors :
Cyrille Lescop، نويسنده , , Holger Herzner، نويسنده , , Hervé Siendt، نويسنده , , Reto Bolliger، نويسنده , , Marco Henneb?hle، نويسنده , , Philipp Weyermann، نويسنده , , Alexandre Briguet، نويسنده , , Isabelle Courdier-Fruh، نويسنده , , Michael Erb، نويسنده , , Mark Foster Gage، نويسنده , , Thomas Meier and Georg Kaim، نويسنده , , Josef P. Magyar، نويسنده , , Andreas von Sprecher، نويسنده ,
Abstract :
Dipeptide-derived α-keto-amide compounds with potent calpain inhibitory activity have been identified. These reversible covalent inhibitors have IC50values down to 25 nM and exhibit greatly improved activity in muscle cells compared to the reference compound MDL28170. Several novel calpain inhibitors have shown positive effects on histological parameters in an animal model of Duchenne muscular dystrophy demonstrating their potential as a treatment option for this fatal disease.
