nature:科学家发现:更好的治疗糖尿病和肥胖症的药物

2018-02-27 佚名 Medicalxpress

Monash University的突破性研究表明,如何“激活”主要糖尿病和肥胖症药物靶点的不同领域,指导未来的药物开发和更好的疾病治疗。

Monash University的突破性研究表明,如何“激活”主要糖尿病和肥胖症药物靶点的不同领域,指导未来的药物开发和更好的疾病治疗。

Monash研究人员已经确定了一个关键药物靶点GLP-1R的特定区域,这些靶点与自然激素和潜在药物的反应有所不同,导致临床前疾病模型产生不同效应。

这一知识可以指导如何改变潜在的新药,以捕获可能更好地治疗疾病的信号的有益差异。

糖尿病是一种广泛传播的慢性疾病,可能导致重大的器官衰竭和死亡,全球范围内影响了近10%的人口,随着肥胖症发病率的增加,这种疾病的发病率也在上升。

常见的糖尿病药物如Byetta和Victoza通过模拟天然激素对该受体起作用而通过GLP-1R受体起作用。靶向GLP-1R的药物也被批准用于治疗肥胖症,并且正在用于治疗包括阿尔茨海默氏病和帕金森病的神经退行性疾病的临床试验。

然而,直到现在,药物和受体之间的相互作用过程仍不清楚。

我们所知道的是,这些药物可以通过GLP-1R产生截然不同的作用,并且这些差异被称为有偏见的激动作用,可导致不同的治疗效果。

最近发现的一种类似药物Byetta的“exendin-P5”是一种“有偏见的激动剂”,因为它与受体的作用不同于目前批准的GLP-1R药物。

最近,Exendin-P5显示降低了糖尿病动物模型中的血糖水平,但是具有与已批准的GLP-1R药物不同的作用方式,最终可以导致更好的患者控制血糖水平的结果。

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