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针对胃泌素治疗胃酸相关疾病和胰腺癌。

Targeting gastrin for the treatment of gastric acid related disorders and pancreatic cancer.

机构信息

Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.

出版信息

Trends Pharmacol Sci. 2011 Apr;32(4):201-5. doi: 10.1016/j.tips.2011.02.003. Epub 2011 Mar 10.

DOI:10.1016/j.tips.2011.02.003
PMID:21397342
Abstract

Gastrin, acting through peripheral cholecystokinin (CCK) 2 receptors, is a major hormonal regulator of gastric acid secretion. The effects of gastrin on acid secretion occur both acutely and chronically because gastrin directly stimulates gastric acid secretion and also exerts trophic effects on the enterochromaffin-like and parietal cells that together constitute the acid secretory apparatus of the stomach. Several antagonists that target the CCK2 receptor have been identified and investigated for the treatment of gastroesophageal reflux disease and pancreatic cancer. In this paper, we discuss the contribution of gastrin to these disease pathologies and the data generated to date from clinical studies investigating CCK2 receptor antagonists.

摘要

胃泌素通过外周胆囊收缩素(CCK)2 受体发挥作用,是胃酸分泌的主要激素调节剂。胃泌素对胃酸分泌的作用既有急性作用,也有慢性作用,因为胃泌素直接刺激胃酸分泌,还对肠嗜铬样细胞和壁细胞发挥营养作用,而这些细胞共同构成了胃的胃酸分泌装置。已经鉴定出几种针对 CCK2 受体的拮抗剂,并对其进行了研究,以治疗胃食管反流病和胰腺癌。在本文中,我们讨论了胃泌素对这些疾病病理的贡献,以及迄今为止从研究 CCK2 受体拮抗剂的临床研究中获得的数据。

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Targeting gastrin for the treatment of gastric acid related disorders and pancreatic cancer.针对胃泌素治疗胃酸相关疾病和胰腺癌。
Trends Pharmacol Sci. 2011 Apr;32(4):201-5. doi: 10.1016/j.tips.2011.02.003. Epub 2011 Mar 10.
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引用本文的文献

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A novel similarity score based on gene ranks to reveal genetic relationships among diseases.一种基于基因排名的新型相似性评分,用于揭示疾病之间的遗传关系。
PeerJ. 2021 Jan 6;9:e10576. doi: 10.7717/peerj.10576. eCollection 2021.
2
Gastrin inhibits gastric cancer progression through activating the ERK-P65-miR23a/27a/24 axis.胃泌素通过激活 ERK-P65-miR23a/27a/24 轴抑制胃癌进展。
J Exp Clin Cancer Res. 2018 Jun 4;37(1):115. doi: 10.1186/s13046-018-0782-7.
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MiR-148a regulates the growth and apoptosis in pancreatic cancer by targeting CCKBR and Bcl-2.
微小RNA-148a通过靶向胆囊收缩素B受体和Bcl-2来调节胰腺癌的生长和凋亡。
Tumour Biol. 2014 Jan;35(1):837-44. doi: 10.1007/s13277-013-1115-2. Epub 2013 Aug 23.
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Gastrin receptor pharmacology.胃泌素受体药理学
Curr Gastroenterol Rep. 2012 Dec;14(6):453-9. doi: 10.1007/s11894-012-0293-1.
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Molecular basis for binding and subtype selectivity of 1,4-benzodiazepine antagonist ligands of the cholecystokinin receptor.胆囊收缩素受体 1,4-苯二氮䓬拮抗剂配体结合和亚型选择性的分子基础。
J Biol Chem. 2012 May 25;287(22):18618-35. doi: 10.1074/jbc.M111.335646. Epub 2012 Mar 30.
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The cholecystokinin CCK2 receptor antagonist, JNJ-26070109, inhibits gastric acid secretion and prevents omeprazole-induced acid rebound in the rat.胆囊收缩素 CCK2 受体拮抗剂 JNJ-26070109 抑制胃酸分泌,并预防大鼠奥美拉唑诱导的胃酸反弹。
Br J Pharmacol. 2012 Jul;166(5):1684-93. doi: 10.1111/j.1476-5381.2012.01878.x.