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Nature Communications:心脏病,一个小分子可能会产生大差别

摘要 : 本期Nature Communications上发表的一项研究显示,被称为BGP-15的一个小分子在关于心脏衰竭的两个小鼠模型中能改善心脏功能。人们希望,该发现将会导致人类心脏病新疗法的开发成功。

 

本期Nature Communications上发表的一项研究显示,被称为BGP-15的一个小分子在关于心脏衰竭的两个小鼠模型中能改善心脏功能。人们希望,该发现将会导致人类心脏病新疗法的开发成功。

心房颤动(最常见的心率异常)和心脏衰竭发病率在增长,但当前的药物疗效有限。Julie McMullen及同事发现,在关于心脏衰竭和心房颤动的小鼠模型中,用BGP-15进行治疗能防止或减少不规则心跳的出现次数,显著改善心脏功能。BGP-15作为其他疾病的一种治疗药物已经进行了人体试验,结果表明其耐受性很好、安全性也很好。

作者还发现,该药物是经由一个出乎意料的分子通道、通过增加对一个被称为“胰岛素样生长因子-1受体”的受体的激发来发挥作用的。这一受体的缺乏此前已被发现与心血管疾病发病风险增大有关。了解BGP-15发挥效应的机制,也许能够进一步帮助心脏病新疗法的开发。

原文标题:The small-molecule ​BGP-15 protects against heart failure and atrial fibrillation in mice

原文摘要:Heart failure (HF) and atrial fibrillation (AF) share common risk factors, frequently coexist and are associated with high mortality. Treatment of HF with AF represents a major unmet need. Here we show that a small molecule, ​BGP-15, improves cardiac function and reduces arrhythmic episodes in two independent mouse models, which progressively develop HF and AF. In these models, ​BGP-15 treatment is associated with increased phosphorylation of the ​insulin-like growth factor 1 receptor (​IGF1R), which is depressed in atrial tissue samples from patients with AF. Cardiac-specific ​IGF1R transgenic overexpression in mice with HF and AF recapitulates the protection observed with ​BGP-15. We further demonstrate that ​BGP-15 and ​IGF1R can provide protection independent of phosphoinositide 3-kinase-Akt and heat-shock protein 70; signalling mediators often defective in the aged and diseased heart. As ​BGP-15 is safe and well tolerated in humans, this study uncovers a potential therapeutic approach for HF and AF.

来源: Nature Communications 浏览次数:74

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