Plos Biology：促进胰岛素分泌，靶向治疗糖尿病新策略

2015-01-26 佚名生物谷

近日，来自荷兰的科学家在国际生物学杂志Plos Biology在线发表了他们的最新研究进展，他们应用结构导向方法设计的cAMP类似物，能够作为Epac2的特异性激动剂激活Epac2，进而促进β胰岛细胞合成分泌胰岛素。这项研究或许可以为通过促进胰岛素分泌的方法治疗糖尿病提供一个可行有效的方案。 cAMP是细胞合成的一种小分子，能够激活细胞内蛋白调控许多生物学过程,包括嗅觉，起搏点活动，调控基因表达

近日，来自荷兰的科学家在国际生物学杂志Plos Biology在线发表了他们的最新研究进展，他们应用结构导向方法设计的cAMP类似物，能够作为Epac2的特异性激动剂激活Epac2，进而促进β胰岛细胞合成分泌胰岛素。这项研究或许可以为通过促进胰岛素分泌的方法治疗糖尿病提供一个可行有效的方案。

cAMP是细胞合成的一种小分子，能够激活细胞内蛋白调控许多生物学过程,包括嗅觉，起搏点活动，调控基因表达，胰岛素分泌以及许多其他过程。在对胰岛素分泌的调控作用中，cAMP能够作用于信号级联途径的不同阶段，调控β胰岛细胞的胰岛素分泌功能。

研究人员通过结构导向的方法设计了cAMP类似物，能够特异性激活cAMP应答蛋白Epac2，激活胰岛素分泌途径的信号级联过程，并且比cAMP具有更强的激活效应。研究人员解析了Epac2与几种cAMP类似物形成的复合体晶体结构，来帮助解释cAMP类似物特异性作用于Epac2并且具有强激活作用的分子基础。除此之外，研究人员还证明，化学合成的cAMP类似物能够促进人胰岛细胞中葡萄糖诱导的胰岛素分泌过程。

综上所述，在该项研究中，研究人员通过结构导向的方法设计合成了cAMP类似物，发现该类似物能够特异性结合Epac2从而激活胰岛素分泌过程中信号级联途径，并通过结构生物学的方法阐述了该类似物作用特异性和强激活作用的分子基础。这一研究成果对开发促胰岛素分泌药物治疗糖尿病具有重要意义。

原始出处

Frank Schwede, Daniela Bertinetti, Carianne N. Langerijs, Michael A. Hadders, Hans Wienk, Johanne H. Ellenbroek, Eelco J. P. de Koning, Johannes L. Bos, Friedrich W. Herberg, Hans-Gottfried Genieser, Richard A. J. Janssen, Holger Rehmann.Structure-Guided Design of Selective Epac1 and Epac2 Agonists Plos Biology 2015

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2015-03-04 sunylz

#Bio#

70 0
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2015-04-22 gwc392

#分泌#

67 0
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2015-02-16 baoya

#胰岛#

72 0
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2015-03-29 12498ebem31暂无昵称

#Biol#

61 0
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2015-04-11 x35042875

AKI对心衰临床治疗意义重大，但依然需要研究检验其适用性

178 0
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2015-01-28 jingyanzhu715_39486101

#胰岛素分泌#

63 0
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2015-01-28 12498568m52暂无昵称

#新策略#

63 0
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2015-01-28 missserena

受益良多，与最近的研究很相近。

146 0
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2015-01-26 223.104.5.**

如果b细胞没有功能了呢

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