Nat Chem Bio：可抑制糖尿病症状的新化合物

2014-01-23 佚名生物谷

据《自然—化学生物学》上一项报告显示，通过对影响细胞内脂质储存的分子进行的表型筛查，科学家检测出了一类可预防小鼠肥胖和糖尿病的合成化合物。这项研究为表型筛查在药物发现方面重新发挥作用提供了一个很好的例子，同时也为治疗代谢综合征提供了潜在的方法。脂质通常以非常特别的方式储存在脂肪细胞中，一旦正常储存出问题，则可能引发Ⅱ型糖尿病。但是，人们对控制脂质储存的机制目前完全不清楚。为了在特定生物分子

据《自然—化学生物学》上一项报告显示，通过对影响细胞内脂质储存的分子进行的表型筛查，科学家检测出了一类可预防小鼠肥胖和糖尿病的合成化合物。这项研究为表型筛查在药物发现方面重新发挥作用提供了一个很好的例子，同时也为治疗代谢综合征提供了潜在的方法。

脂质通常以非常特别的方式储存在脂肪细胞中，一旦正常储存出问题，则可能引发Ⅱ型糖尿病。但是，人们对控制脂质储存的机制目前完全不清楚。

为了在特定生物分子目标位置的情况下找到能够影响该机制的化合物，Enrique Saez、 Benjamin Cravatt等人对脂肪细胞分化进行了表型筛查。所使用的化合物可以抑制丝氨酸水解酶——一类对一系列细胞生化反应过程起着重要作用的酶。研究人员在细胞培养中发现两种化合物的目标是一种被称为羧酸酯酶-3的丝氨酸水解酶。这两种化合物的应用可抑制小鼠模型中的糖尿病和肥胖症状。这些发现首次为羧酸酯酶-3在脂质分解中所起的作用提供了化学证据，同时也为代谢紊乱的治疗提供了一种可能。

原文出处：

Eduardo Dominguez, Andrea Galmozzi, Jae Won Chang, Ku-Lung Hsu, Joanna Pawlak, Weiwei Li, Cristina Godio, Jason Thomas, David Partida, Sherry Niessen, Paul E O'Brien, Aaron P Russell, Matthew J Watt, Daniel K Nomura, Benjamin F Cravatt & Enrique Saez. Integrated phenotypic and activity-based profiling links Ces3 to obesity and diabetes. Nature Chemical Biology, 22 December 2013

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2014-08-20 wangyang7958

#化合物#

107 0
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2014-12-26 liye789132251

#Nat#

93 0
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2014-12-02 sunylz

#Bio#

89 0
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2014-01-24 lifefamily

很多药物认识都是一个漫长的过程！

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