Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy.

Lescop C; Herzner H; Siendt H; Bolliger R; Hennebohle M; Weyermann P; Briguet A; Courdier Fruh I; Erb M; Foster M; Meier T; Magyar JP; von Sprecher A

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Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy.

机译：新型细胞穿透性α-酮酰胺钙蛋白酶抑制剂可作为肌营养不良症的潜在治疗方法。

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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.

机译：已经鉴定出具有强钙蛋白酶抑制活性的二肽衍生的α-酮酰胺化合物。与参考化合物MDL28170相比，这些可逆共价抑制剂的IC（50）值低至25nM，并且在肌肉细胞中表现出大大改善的活性。几种新型钙蛋白酶抑制剂已在Duchenne肌营养不良症动物模型中显示出对组织学参数的积极影响，表明了其作为这种致命疾病的治疗选择的潜力。

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《Bioorganic and Medicinal Chemistry Letters》 |2005年第23期|共6页
作者
Lescop C; Herzner H; Siendt H; Bolliger R; Hennebohle M; Weyermann P; Briguet A; Courdier Fruh I; Erb M; Foster M; Meier T; Magyar JP; von Sprecher A;
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正文语种 eng
中图分类基础医学;
关键词
calpain inhibitors; therapeutic aspects; Amides; penetratin; g lt; 3gt; 酰胺类;

机译：calpain inhibitors;therapeutic aspects;Amides;penetratin;g 3;酰胺类;

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1. Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy. [J] . Lescop C, Herzner H, Siendt H, Bioorganic and Medicinal Chemistry Letters . 2005,第23期

机译：新型细胞穿透性α-酮酰胺钙蛋白酶抑制剂可作为肌营养不良症的潜在治疗方法。
2. Angiotensin-converting-enzyme inhibitors versus steroids as first-line drug treatment in Duchenne muscular dystrophy. [J] . Chabrier S, Desguerre I, Porte M, Developmental Medicine and Child Neurology . 2010,第11期

机译：血管紧张素转换酶抑制剂与类固醇激素是杜兴肌营养不良症的一线药物治疗。
3. Evaluation of potential synergistic action of a combined treatment with alpha-methyl-prednisolone and taurine on the mdx mouse model of Duchenne muscular dystrophy. [J] . Cozzoli A, Rolland JF, Capogrosso RF, Neuropathology and applied neurobiology . 2011,第3期

机译：评估α-甲基强的松龙和牛磺酸联合治疗对Duchenne肌营养不良症的mdx小鼠模型的潜在协同作用。
4. Investigations into the potential of the calpain 2 inhibitor, SJA6017, to retard cataract [C] . Suman Biswas, Fred Harris, Sarah Dennison, 2006年第二届上海国际生理生物物理大学 . 2006

机译：研究钙蛋白酶2抑制剂SJA6017延缓白内障的潜力
5. The role of satellite cells in skeletal muscle revascularization: A potential factor in muscular dystrophy. [D] . Flann, Kyle L. 2010

机译：卫星细胞在骨骼肌血运重建中的作用：肌营养不良的潜在因素。
6. Histone deacetylase inhibitors as potential treatment for spinal muscular atrophy [O] . Jafar Mohseni, Z.A.M.H. Zabidi-Hussin, Teguh Haryo Sasongko 2019

机译：组蛋白脱乙酰基酶抑制剂可治疗脊髓性肌萎缩症
7. Evaluation of potential synergistic action of a combined treatment with alpha-methyl-prednisolone and taurine on the mdx mouse model of Duchenne muscular dystrophy. [O] . Cozzoli A, Rolland JF, Capogrosso RF, 2011

机译：评价联合治疗与α-甲基强的松龙和牛磺酸对Duchenne肌营养不良症的mdx小鼠模型的潜在协同作用。
8. Evaluation of MMX1902 as an Oral Treatment for Duchenne Muscular Dystrophy. [R] . Rodgers, K. E. 2016

机译：mmX1902作为Duchenne肌营养不良症口服治疗的评价。

Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy.

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