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Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy |
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| Authors: | Lescop Cyrille Herzner Holger Siendt Hervé Bolliger Reto Henneböhle Marco Weyermann Philipp Briguet Alexandre Courdier-Fruh Isabelle Erb Michael Foster Mark Meier Thomas Magyar Josef P von Sprecher Andreas |
| Institution: | Medicinal Chemistry Department, Santhera Pharmaceuticals, Hammerstrasse 25, CH-4410 Liestal, Switzerland. cyrille.lescop@santhera.com |
| 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. |
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