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2
Farnesoid X receptor induces Takeda G-protein receptor 5 cross-talk to regulate bile acid synthesis and hepatic metabolism.法尼酯X受体诱导武田G蛋白偶联受体5相互作用以调节胆汁酸合成和肝脏代谢。
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Drug Discov Today. 2009 May;14(9-10):523-30. doi: 10.1016/j.drudis.2009.02.005. Epub 2009 Feb 25.
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G-protein-coupled bile acid receptor plays a key role in bile acid metabolism and fasting-induced hepatic steatosis in mice.G蛋白偶联胆汁酸受体在小鼠胆汁酸代谢和禁食诱导的肝脂肪变性中起关键作用。
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Total -2 Palmitic Triacylglycerols and the Ratio of OPL to OPO in Human Milk Fat Substitute Modulated Bile Acid Metabolism and Intestinal Microbiota Composition in Rats.总-2 棕榈酸三酰甘油和人乳脂肪替代物中 OPL 与 OPO 的比例调节大鼠胆汁酸代谢和肠道微生物组成。
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本文引用的文献

1
Chronic fibrosing cholangiopathies: a consequence of a defective HCO₃⁻ "umbrella"?慢性纤维性胆管病:HCO₃⁻“保护伞”缺陷的后果?
Clin Res Hepatol Gastroenterol. 2011 Feb;35(2):85-8. doi: 10.1016/j.clinre.2010.10.005.
2
Immediate neuroendocrine signaling after partial hepatectomy through acute portal hyperpressure and cholestasis.部分肝切除术后通过急性门脉高压和胆汁淤积的即刻神经内分泌信号转导。
J Hepatol. 2011 Mar;54(3):481-8. doi: 10.1016/j.jhep.2010.07.012. Epub 2010 Sep 22.
3
Mutational characterization of the bile acid receptor TGR5 in primary sclerosing cholangitis.原发性硬化性胆管炎中胆汁酸受体 TGR5 的突变特征。
PLoS One. 2010 Aug 25;5(8):e12403. doi: 10.1371/journal.pone.0012403.
4
Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor and TGR5 agonist.半合成胆酸衍生物 INT-767 的功能特征,一种双重法尼醇 X 受体和 TGR5 激动剂。
Mol Pharmacol. 2010 Oct;78(4):617-30. doi: 10.1124/mol.110.064501. Epub 2010 Jul 14.
5
The membrane-bound bile acid receptor TGR5 (Gpbar-1) is localized in the primary cilium of cholangiocytes.膜结合胆汁酸受体 TGR5(Gpbar-1)定位于胆管细胞的初级纤毛中。
Biol Chem. 2010 Jul;391(7):785-9. doi: 10.1515/BC.2010.077.
6
Synthesis and structure-activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists.合成及结构活性关系的一系列 3-芳基-4-异恶唑甲酰胺作为一类新的 TGR5 激动剂。
Bioorg Med Chem Lett. 2010 Feb 15;20(4):1363-7. doi: 10.1016/j.bmcl.2010.01.003. Epub 2010 Jan 7.
7
Bile acid-activated receptors in the treatment of dyslipidemia and related disorders.胆汁酸激活受体在血脂异常及相关疾病治疗中的作用。
Prog Lipid Res. 2010 Apr;49(2):171-85. doi: 10.1016/j.plipres.2009.11.001. Epub 2009 Dec 2.
8
Bile-acid-activated receptors: targeting TGR5 and farnesoid-X-receptor in lipid and glucose disorders.胆汁酸激活受体:在脂质和葡萄糖代谢紊乱中靶向 TGR5 和法尼醇 X 受体。
Trends Pharmacol Sci. 2009 Nov;30(11):570-80. doi: 10.1016/j.tips.2009.08.001. Epub 2009 Sep 14.
9
TGR5-mediated bile acid sensing controls glucose homeostasis.TGR5介导的胆汁酸感知调控葡萄糖稳态。
Cell Metab. 2009 Sep;10(3):167-77. doi: 10.1016/j.cmet.2009.08.001.
10
Preliminary report: genetic variation within the GPBAR1 gene is not associated with metabolic traits in white subjects at an increased risk for type 2 diabetes mellitus.初步报告:在2型糖尿病风险增加的白人受试者中,GPBAR1基因内的遗传变异与代谢性状无关。
Metabolism. 2009 Dec;58(12):1809-11. doi: 10.1016/j.metabol.2009.06.012. Epub 2009 Aug 28.

TGR5:体重维持和葡萄糖代谢的新靶点。

TGR5: a novel target for weight maintenance and glucose metabolism.

作者信息

Chen Xiaosong, Lou Guiyu, Meng Zhipeng, Huang Wendong

机构信息

Division of Gene Regulation and Drug Discovery, Beckman Research Institute, City of Hope National Medical Center, 1500 East Duarte Road, Duarte, CA 91010, USA.

出版信息

Exp Diabetes Res. 2011;2011:853501. doi: 10.1155/2011/853501. Epub 2011 Jun 21.

DOI:10.1155/2011/853501
PMID:21754919
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3132465/
Abstract

TGR5, an emerging G protein-coupled receptor, was identified as a membrane receptor for bile acids. The expression of TGR5 and its function are distinct from the previously identified nuclear bile acid receptor, farnesoid X receptor (FXR). These two bile acid receptors complement with each other for maintaining bile acid homeostasis and mediating bile acid signaling. Both receptors are also shown to play roles in regulating inflammation and glucose metabolism. An interesting finding for TGR5 is its role in energy metabolism. The discovery of TGR5 expression in brown adipocyte tissues (BATs) and the recent demonstration of BAT in adult human body suggest a potential approach to combat obesity by targeting TGR5 to increase thermogenesis. We summarize here the latest finding of TGR5 research, especially its role in energy metabolism and glucose homeostasis.

摘要

TGR5是一种新发现的G蛋白偶联受体,被确定为胆汁酸的膜受体。TGR5的表达及其功能与先前鉴定的核胆汁酸受体法尼醇X受体(FXR)不同。这两种胆汁酸受体相互补充,以维持胆汁酸稳态并介导胆汁酸信号传导。这两种受体还显示在调节炎症和葡萄糖代谢中发挥作用。TGR5的一个有趣发现是其在能量代谢中的作用。在棕色脂肪组织(BATs)中发现TGR5表达,以及最近在成人体内发现BAT,提示了一种通过靶向TGR5以增加产热来对抗肥胖的潜在方法。我们在此总结TGR5研究的最新发现,特别是其在能量代谢和葡萄糖稳态中的作用。