Document Report Card
Basic Information
ID: ALA1141207
Journal: Bioorg Med Chem Lett
Title: Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy.
Authors: Lescop C, Herzner H, Siendt H, Bolliger R, Henneböhle M, Weyermann P, Briguet A, Courdier-Fruh I, Erb M, Foster M, Meier T, Magyar JP, von Sprecher A.
Abstract: Dipeptide-derived alpha-keto-amide compounds with potent calpain inhibitory activity have been identified. These reversible covalent inhibitors have IC(50) values down to 25nM 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.
CiteXplore: 16185867