Human GIP(3-30)NH2 inhibits G protein-dependent as well as G protein-independent signaling and is selective for the GIP receptor with high-affinity binding to primate but not rodent GIP receptors

Gabe Maria Buur Nordskov; Sparre-Ulrich Alexander Hovard; Pedersen Mie Fabricius; Gasbjerg Laerke Smidt; Inoue Asuka; Brauner-Osborne Hans; Hartmann Bolette; Rosenkilde Mette Marie

首页> 外文期刊>Biochemical Pharmacology >Human GIP(3-30)NH2 inhibits G protein-dependent as well as G protein-independent signaling and is selective for the GIP receptor with high-affinity binding to primate but not rodent GIP receptors

【24h】

Human GIP(3-30)NH2 inhibits G protein-dependent as well as G protein-independent signaling and is selective for the GIP receptor with high-affinity binding to primate but not rodent GIP receptors

机译：人的GIP（3-30）NH2抑制G蛋白依赖性以及G蛋白无关的信号传导，并选择具有高亲和力与灵长类动物的高亲和力结合的GIP受体的选择性，但不是啮齿动物的GIP受体

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

GIP(3-30)NH2 is a high affinity antagonist of the GIP receptor (GIPR) in humans inhibiting insulin secretion via G protein-dependent pathways. However, its ability to inhibit G protein-independent signaling is unknown. Here we determine its action on arrestin-recruitment and receptor internalization in recombinant cells. As GIP is adipogenic, we evaluate the inhibitory actions of GIP(3-30)NH2 in human adipocytes. Finally, we determine the receptor selectivity of GIP(3-30)NH2 among other human and animal GPCRs.

机译：GIP（3-30）NH2是人类抑制胰岛素分泌物的巨大胶质受体（GIPR）的高亲和力拮抗剂，抑制通过G蛋白依赖性途径。然而，它抑制无关的信令的能力是未知的。在这里，我们确定其对重组细胞中诱导患者和受体内化的作用。由于GIP是脂肪发生的，我们评估吉普（3-30）NH2在人脂肪细胞中的抑制作用。最后，我们确定其他人和动物GPCR中GIP（3-30）NH2的受体选择性。

著录项

来源
《Biochemical Pharmacology》 |2018年第2018期|共11页
作者
Gabe Maria Buur Nordskov; Sparre-Ulrich Alexander Hovard; Pedersen Mie Fabricius; Gasbjerg Laerke Smidt; Inoue Asuka; Brauner-Osborne Hans; Hartmann Bolette; Rosenkilde Mette Marie;
展开▼
作者单位

Univ Copenhagen Fac Hlth &

Med Sci Dept Biomed Sci Copenhagen Denmark;

Antag Therapeut ApS Copenhagen Denmark;

Univ Copenhagen Fac Hlth &

Med Sci Dept Drug Design &

Pharmacol Copenhagen Denmark;

Univ Copenhagen Fac Hlth &

Med Sci Dept Biomed Sci Copenhagen Denmark;

Tohoku Univ Grad Sch Pharmaceut Sci Lab Mol &

Cellular Biochem Sendai Miyagi Japan;

Univ Copenhagen Fac Hlth &

Med Sci Dept Drug Design &

Pharmacol Copenhagen Denmark;

Univ Copenhagen Fac Hlth &

Med Sci Dept Biomed Sci Copenhagen Denmark;

Univ Copenhagen Fac Hlth &

Med Sci Dept Biomed Sci Copenhagen Denmark;

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类药理学;
关键词
Glucose-dependent insulinotropic polypeptide (GIP); GIP receptor; Antagonist; Human subcutaneous adipocytes; Signaling;

机译：葡萄糖依赖性胰岛素多肽（GIP）;GIP受体;拮抗剂;人皮下脂肪细胞;信号;

相似文献

外文文献
中文文献
专利

1. Inhibition of histamine receptor H3 suppresses the growth and metastasis of human non-small cell lung cancer cells via inhibiting PI3K/Akt/mTOR and MEK/ERK signaling pathways and blocking EMT [J] . Yan-yan Zhao, Shi-rong Zhang, Jing Jia, 中国药理学报：英文版 . 2021,第008期
2. Human GIP(3-30)NH2 inhibits G protein-dependent as well as G protein-independent signaling and is selective for the GIP receptor with high-affinity binding to primate but not rodent GIP receptors [J] . Gabe Maria Buur Nordskov, Sparre-Ulrich Alexander Hovard, Pedersen Mie Fabricius, Biochemical Pharmacology . 2018,第期

机译：人的GIP（3-30）NH2抑制G蛋白依赖性以及G蛋白无关的信号传导，并且对GIP受体选择具有高亲和力与灵长类动物的结合但不是啮齿动物覆盖物受体的选择性
3. GIP(3-30)NH2 is a potent competitive antagonist of the GIP receptor and effectively inhibits GIP-mediated insulin, glucagon, and somatostatin release [J] . Sparre-Ulrich A. H., Gabe M. N., Gasbjerg L. S., Biochemical Pharmacology . 2017,第期

机译：GIP（3-30）NH2是一种巨大的巨大态竞争对手，有效地抑制GIP介导的胰岛素，胰高血糖素和生长抑素释放
4. Dose-dependent efficacy of the glucose-dependent insulinotropic polypeptide (GIP) receptor antagonist GIP(3-30) NH2 on GIP actions in humans [J] . L?rke Smidt Gasbjerg, Emilie J. Bari, Signe Stensen, Diabetes, obesity & metabolism . 2021,第1期

机译：葡萄糖依赖性胰岛素多肽（GIP）受体拮抗剂GIP（3-30）NH2对人类的GIP作用的剂量依赖性疗效
5. Development of a mAb Binding a Conformational Epitope on Human and Rodent Insulin Receptor Using a Naive Antibody Yeast Display Library [C] . Morten Gronbech Rasch, Rita Slaaby, Niels Blume Protein Engineering Summit. . 2018

机译：使用Naive抗体酵母显示文库在人和啮齿动物胰岛素受体上结合构象表位的MAB
6. Alternative signaling pathways of the glucose -dependent insulinotropic polypeptide (GIP) receptor. [D] . Ehses, Jan A. 2003

机译：葡萄糖依赖性促胰岛素多肽（GIP）受体的替代信号通路。
7. Species‐specific action of (Pro3)GIP – a full agonist at human GIP receptors but a partial agonist and competitive antagonist at rat and mouse GIP receptors [O] . A H Sparre‐Ulrich, †, L S Hansen, 2016

机译：（Pro3）GIP的物种特异性作用–对人GIP受体的完全激动剂但对大鼠和小鼠GIP受体的部分激动剂和竞争性拮抗剂
8. GIP(3-30)NH2 is an efficacious GIP receptor antagonist in humans: a randomised, double-blinded, placebo-controlled, crossover study [O] . Lærke S. Gasbjerg, Mikkel B. Christensen, Bolette Hartmann, 2017

机译：GIP（3-30）NH2是人类有效的盖皮克受体拮抗剂：随机，双盲，安慰剂控制，交叉研究
9. Short-Term Desensitization of Muscarinic Cholinergic Receptors in Mouse Neuroblastoma Cells: Selective Loss of Agonist Low-Affinity and Pirenzepine High-Affinity Binding Sites [R] . Cioffi, C. L., El-Fakahany, E. E. 1986

机译：小鼠神经母细胞瘤细胞中毒蕈碱胆碱能受体的短期脱敏：激动剂低亲和力和哌仑西平高亲和力结合位点的选择性丧失

Human GIP(3-30)NH2 inhibits G protein-dependent as well as G protein-independent signaling and is selective for the GIP receptor with high-affinity binding to primate but not rodent GIP receptors

摘要

著录项

相似文献

相关主题

期刊订阅