کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1367712 | 981645 | 2005 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Novel cell-penetrating α-keto-amide calpain inhibitors as potential treatment for muscular dystrophy
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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![عکس صفحه اول مقاله: Novel cell-penetrating α-keto-amide calpain inhibitors as potential treatment for muscular dystrophy Novel cell-penetrating α-keto-amide calpain inhibitors as potential treatment for muscular dystrophy](/preview/png/1367712.png)
چکیده انگلیسی
Dipeptide-derived α-keto-amide compounds with potent calpain inhibitory activity have been identified. These reversible covalent inhibitors have IC50 values 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.
The synthesis of novel α-keto-amide calpain inhibitors bearing a lipoyl residue is reported. They demonstrated an improved activity in muscle cells compared to MDL28170, referring to increased cell membrane permeability.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 23, 1 December 2005, Pages 5176–5181
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 23, 1 December 2005, Pages 5176–5181
نویسندگان
Cyrille Lescop, Holger Herzner, Hervé Siendt, Reto Bolliger, Marco Henneböhle, Philipp Weyermann, Alexandre Briguet, Isabelle Courdier-Fruh, Michael Erb, Mark Foster, Thomas Meier, Josef P. Magyar, Andreas von Sprecher,