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本文引用的文献

1
Unraveling the science of incretin biology.解析肠促胰岛素生物学的科学原理。
Am J Med. 2009 Jun;122(6 Suppl):S3-S10. doi: 10.1016/j.amjmed.2009.03.012.
2
Islet G protein-coupled receptors as potential targets for treatment of type 2 diabetes.胰岛G蛋白偶联受体作为2型糖尿病治疗的潜在靶点。
Nat Rev Drug Discov. 2009 May;8(5):369-85. doi: 10.1038/nrd2782. Epub 2009 Apr 14.
3
Enhanced Rap1 activation and insulin secretagogue properties of an acetoxymethyl ester of an Epac-selective cyclic AMP analog in rat INS-1 cells: studies with 8-pCPT-2'-O-Me-cAMP-AM.Epac 选择性环磷酸腺苷类似物的乙酰氧基甲酯在大鼠 INS-1 细胞中增强 Rap1 激活及胰岛素促分泌特性：8-对氯苯硫基-2'-O-甲基环磷酸腺苷-乙酰氧基甲酯的研究
J Biol Chem. 2009 Apr 17;284(16):10728-36. doi: 10.1074/jbc.M900166200. Epub 2009 Feb 25.
4
Kinetics of Rab27a-dependent actions on vesicle docking and priming in pancreatic beta-cells.Rab27a对胰腺β细胞中囊泡对接和启动的依赖性作用的动力学
J Physiol. 2008 Nov 15;586(22):5367-81. doi: 10.1113/jphysiol.2008.158477. Epub 2008 Sep 18.
5
8-pCPT-2'-O-Me-cAMP-AM: an improved Epac-selective cAMP analogue.8-对氯苯硫酚-2'-O-甲基环磷酸腺苷-酰胺：一种改进的Epac选择性环磷酸腺苷类似物。
Chembiochem. 2008 Sep 1;9(13):2052-4. doi: 10.1002/cbic.200800216.
6
Role of the cAMP sensor Epac as a determinant of KATP channel ATP sensitivity in human pancreatic beta-cells and rat INS-1 cells.环磷酸腺苷（cAMP）传感器交换蛋白直接激活cAMP（Epac）作为人胰岛β细胞和大鼠胰岛瘤INS-1细胞中ATP敏感性钾通道（KATP通道）ATP敏感性决定因素的作用。
J Physiol. 2008 Mar 1;586(5):1307-19. doi: 10.1113/jphysiol.2007.143818. Epub 2008 Jan 17.
7
Essential role of Epac2/Rap1 signaling in regulation of insulin granule dynamics by cAMP.Epac2/Rap1信号通路在cAMP调节胰岛素颗粒动力学中的重要作用。
Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19333-8. doi: 10.1073/pnas.0707054104. Epub 2007 Nov 26.
8
Synchronizing Ca2+ and cAMP oscillations in pancreatic beta-cells: a role for glucose metabolism and GLP-1 receptors? Focus on "regulation of cAMP dynamics by Ca2+ and G protein-coupled receptors in the pancreatic beta-cell: a computational approach".胰腺β细胞中Ca2+与cAMP振荡的同步：葡萄糖代谢和胰高血糖素样肽-1受体的作用？聚焦于“胰腺β细胞中Ca2+和G蛋白偶联受体对cAMP动力学的调节：一种计算方法”
Am J Physiol Cell Physiol. 2008 Jan;294(1):C4-6. doi: 10.1152/ajpcell.00522.2007. Epub 2007 Nov 7.
9
Activation of exchange protein directly activated by cyclic adenosine monophosphate and protein kinase A regulate common and distinct steps in promoting plasma membrane exocytic and granule-to-granule fusions in rat islet beta cells.由环磷酸腺苷直接激活的交换蛋白和蛋白激酶A的激活调节大鼠胰岛β细胞中促进质膜胞吐和颗粒间融合的共同和不同步骤。
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10
Epac-selective cAMP analogs: new tools with which to evaluate the signal transduction properties of cAMP-regulated guanine nucleotide exchange factors.Epac 选择性 cAMP 类似物：用于评估 cAMP 调节的鸟嘌呤核苷酸交换因子信号转导特性的新工具。
Cell Signal. 2008 Jan;20(1):10-20. doi: 10.1016/j.cellsig.2007.07.009. Epub 2007 Jul 25.

Epac 激活剂 8-pCPT-2'-O-Me-cAMP-AM 依赖葡萄糖增强小鼠胰岛胰岛素分泌。

Glucose-dependent potentiation of mouse islet insulin secretion by Epac activator 8-pCPT-2'-O-Me-cAMP-AM.

机构信息

Department of Medicine, State University of New York Upstate Medical University Syracuse, NY, USA.

出版信息

Islets. 2009 Nov-Dec;1(3):260-5. doi: 10.4161/isl.1.3.9645.

DOI:10.4161/isl.1.3.9645
PMID:21099281
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2859731/
Abstract

Epac2 is a cAMP-regulated guanine nucleotide exchange factor (cAMP-GEF) that is proposed to mediate stimulatory actions of the second messenger cAMP on mouse islet insulin secretion. Here we have used methods of islet perifusion to demonstrate that the acetoxymethyl ester (AM-ester) of an Epac-selective cAMP analog (ESCA) penetrates into mouse islets and is capable of potentiating both first and second phases of glucose-stimulated insulin secretion (GSIS). When used at low concentrations (1-10 μM), 8-pCPT-2'-O-Me-cAMP-AM activates Rap1 GTPase but exhibits little or no ability to activate protein kinase A (PKA), as validated in assays of in vitro PKA activity (phosphorylation of Kemptide), Ser (133) CREB phosphorylation status, RIP1-CRE-Luc reporter gene activity, and PKA-dependent AKAR3 biosensor activation. Since quantitative PCR demonstrates Epac2 mRNA to be expressed at levels ca. 5.3-fold greater than that of Epac1, available evidence indicates that Epac2 does in fact mediate stimulatory actions of cAMP on mouse islet GSIS.

摘要

Epac2 是一种 cAMP 调节的鸟嘌呤核苷酸交换因子（cAMP-GEF），据推测它介导第二信使 cAMP 对小鼠胰岛胰岛素分泌的刺激作用。在这里，我们使用胰岛灌流的方法证明，Epac 选择性 cAMP 类似物（ESCA）的乙酰氧甲基酯（AM-ester）能够渗透到小鼠胰岛中，并能够增强葡萄糖刺激的胰岛素分泌（GSIS）的第一和第二阶段。当使用低浓度（1-10 μM）时，8-pCPT-2'-O-Me-cAMP-AM 激活 Rap1 GTPase，但几乎没有或没有能力激活蛋白激酶 A（PKA），如体外 PKA 活性测定（Kemptide 磷酸化）、Ser（133）CREB 磷酸化状态、RIP1-CRE-Luc 报告基因活性和 PKA 依赖性 AKAR3 生物传感器激活所验证。由于定量 PCR 表明 Epac2 mRNA 的表达水平约为 Epac1 的 5.3 倍，现有证据表明 Epac2 确实介导 cAMP 对小鼠胰岛 GSIS 的刺激作用。