• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

尾加压素 II 配体：从肽类结构到非肽类结构的概述

Urotensin-II Ligands: An Overview from Peptide to Nonpeptide Structures.

作者信息

Merlino Francesco, Di Maro Salvatore, Munaim Yousif Ali, Caraglia Michele, Grieco Paolo

机构信息

Department of Pharmacy, University of Naples Federico II, 80131 Naples, Italy.

出版信息

J Amino Acids. 2013;2013:979016. doi: 10.1155/2013/979016. Epub 2013 Feb 25.

DOI:10.1155/2013/979016
PMID:23533711
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3596952/
Abstract

Urotensin-II was originally isolated from the goby urophysis in the 1960s as a vasoactive peptide with a prominent role in cardiovascular homeostasis. The identification of human isoform of urotensin-II and its specific UT receptor by Ames et al. in 1999 led to investigating the putative role of the interaction U-II/UT receptor in multiple pathophysiological effects in humans. Since urotensin-II is widely expressed in several peripheral tissues including cardiovascular system, the design and development of novel urotensin-II analogues can improve knowledge about structure-activity relationships (SAR). In particular, since the modulation of the U-II system offers a great potential for therapeutic strategies related to the treatment of several diseases, like cardiovascular diseases, the research of selective and potent ligands at UT receptor is more fascinating. In this paper, we review the developments of peptide and nonpeptide U-II structures so far developed in order to contribute also to a more rational and detectable design and synthesis of new molecules with high affinity at the UT receptor.

摘要

尾加压素II最初于20世纪60年代从虎鱼的尾垂体中分离出来，是一种血管活性肽，在心血管稳态中起重要作用。1999年，艾姆斯等人鉴定出人类尾加压素II同工型及其特异性UT受体，从而开始研究U-II/UT受体相互作用在人类多种病理生理效应中的假定作用。由于尾加压素II在包括心血管系统在内的多个外周组织中广泛表达，新型尾加压素II类似物的设计和开发可以增进对构效关系（SAR）的了解。特别是，由于U-II系统的调节为与多种疾病（如心血管疾病）治疗相关的治疗策略提供了巨大潜力，因此对UT受体选择性和强效配体的研究更具吸引力。在本文中，我们回顾了迄今为止已开发的肽类和非肽类U-II结构的进展，以便也有助于更合理和可检测地设计和合成对UT受体具有高亲和力的新分子。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/aa3b098e3ea1/JAA2013-979016.012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/9bbd5748f39f/JAA2013-979016.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/56ad67594a77/JAA2013-979016.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/c1ac713fad52/JAA2013-979016.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/a800a444c247/JAA2013-979016.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/74b82e42b619/JAA2013-979016.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/aaa80a92645b/JAA2013-979016.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/1cc532eab292/JAA2013-979016.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/603edd88c4a2/JAA2013-979016.008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/31ed6a03bf31/JAA2013-979016.009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/ca64124c9218/JAA2013-979016.010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/cd169cfd3608/JAA2013-979016.011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/aa3b098e3ea1/JAA2013-979016.012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/9bbd5748f39f/JAA2013-979016.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/56ad67594a77/JAA2013-979016.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/c1ac713fad52/JAA2013-979016.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/a800a444c247/JAA2013-979016.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/74b82e42b619/JAA2013-979016.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/aaa80a92645b/JAA2013-979016.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/1cc532eab292/JAA2013-979016.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/603edd88c4a2/JAA2013-979016.008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/31ed6a03bf31/JAA2013-979016.009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/ca64124c9218/JAA2013-979016.010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/cd169cfd3608/JAA2013-979016.011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8f7/3596952/aa3b098e3ea1/JAA2013-979016.012.jpg

相似文献

1
Urotensin-II Ligands: An Overview from Peptide to Nonpeptide Structures.尾加压素 II 配体：从肽类结构到非肽类结构的概述
J Amino Acids. 2013;2013:979016. doi: 10.1155/2013/979016. Epub 2013 Feb 25.
2
Urotensin-II receptor antagonists.尾加压素 II 受体拮抗剂
Curr Med Chem. 2006;13(3):267-75. doi: 10.2174/092986706775476061.
3
Identification of novel Urotensin-II receptor antagonists with potent inhibition of U-II induced pressor response in mice.新型尿钠肽- II受体拮抗剂的鉴定及其对小鼠尿钠肽- II诱导的升压反应的强效抑制作用。
Eur J Pharmacol. 2020 Nov 5;886:173391. doi: 10.1016/j.ejphar.2020.173391. Epub 2020 Aug 1.
4
International Union of Basic and Clinical Pharmacology. XCII. Urotensin II, urotensin II-related peptide, and their receptor: from structure to function.国际基础与临床药理学联盟. XCII. 尾加压素 II、尾加压素 II 相关肽及其受体：从结构到功能。
Pharmacol Rev. 2015;67(1):214-58. doi: 10.1124/pr.114.009480.
5
Increased expression of urotensin II, urotensin II-related peptide and urotensin II receptor mRNAs in the cardiovascular organs of hypertensive rats: comparison with endothelin-1.高血压大鼠心血管器官中尾加压素II、尾加压素II相关肽及尾加压素II受体mRNA表达增加：与内皮素-1的比较
Peptides. 2009 Jun;30(6):1124-9. doi: 10.1016/j.peptides.2009.02.009. Epub 2009 Feb 21.
6
Role of urotensin II in peripheral tissue as an autocrine/paracrine growth factor.尾加压素II在外周组织中作为自分泌/旁分泌生长因子的作用。
Peptides. 2004 Oct;25(10):1775-81. doi: 10.1016/j.peptides.2004.03.028.
7
Recent structure-activity studies of the peptide hormone urotensin-II, a potent vasoconstrictor.最近对肽激素尾加压素II（一种有效的血管收缩剂）的构效关系研究。
Curr Med Chem. 2004 Apr;11(8):969-79. doi: 10.2174/0929867043455495.
8
The role of urotensin II in cardiovascular and renal physiology and diseases.尾加压素II在心血管和肾脏生理及疾病中的作用。
Br J Pharmacol. 2006 Aug;148(7):884-901. doi: 10.1038/sj.bjp.0706800. Epub 2006 Jun 19.
9
Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin System.尾加压素 II 受体拮抗剂帕罗苏兰（ACT-058362；1-[2-(4-苄基-4-羟基-哌啶-1-基)-乙基]-3-(2-甲基-喹啉-4-基)-脲硫酸盐）的药理学：首次证明尾加压素系统的病理生理作用
J Pharmacol Exp Ther. 2004 Oct;311(1):204-12. doi: 10.1124/jpet.104.068320. Epub 2004 May 14.
10
Structure-activity relationships of urotensin II and URP.尾加压素II与尾加压素相关肽的构效关系。
Peptides. 2008 May;29(5):658-73. doi: 10.1016/j.peptides.2007.08.014. Epub 2007 Aug 19.

引用本文的文献

1
Urotensin-II-Targeted Liposomes as a New Drug Delivery System towards Prostate and Colon Cancer Cells.靶向尿紧张素II的脂质体作为一种针对前列腺癌细胞和结肠癌细胞的新型药物递送系统
J Oncol. 2019 Dec 17;2019:9293560. doi: 10.1155/2019/9293560. eCollection 2019.
2
Understanding Peptide Binding in Class A G Protein-Coupled Receptors.了解 A 类 G 蛋白偶联受体中的肽结合。
Mol Pharmacol. 2019 Nov;96(5):550-561. doi: 10.1124/mol.119.115915. Epub 2019 Jul 10.
3
A new therapeutic approach to erectile dysfunction: urotensin-II receptor high affinity agonist ligands.

本文引用的文献

1
Endogenous urotensin II selectively modulates erectile function through eNOS.内源性尾加压素 II 通过 eNOS 选择性调节勃起功能。
PLoS One. 2012;7(2):e31019. doi: 10.1371/journal.pone.0031019. Epub 2012 Feb 2.
2
Urocontrin, a novel UT receptor ligand with a unique pharmacological profile.尿路上皮素，一种具有独特药理学特性的新型 UT 受体配体。
Biochem Pharmacol. 2012 Mar 1;83(5):608-15. doi: 10.1016/j.bcp.2011.12.009. Epub 2011 Dec 16.
3
The vasoactive peptides urotensin II and urotensin II-related peptide regulate astrocyte activity through common and distinct mechanisms: involvement in cell proliferation.
勃起功能障碍的一种新治疗方法：尾加压素 II 受体高亲和力激动剂配体
Asian J Androl. 2015 Jan-Feb;17(1):81-5. doi: 10.4103/1008-682X.133322.
4
Urotensin II receptor determines prognosis of bladder cancer regulating cell motility/invasion.尾加压素II受体通过调节细胞运动/侵袭来决定膀胱癌的预后。
J Exp Clin Cancer Res. 2014 Jun 3;33(1):48. doi: 10.1186/1756-9966-33-48.
血管活性肽尾加压素 II 和尾加压素 II 相关肽通过共同和不同的机制调节星形胶质细胞活性：参与细胞增殖。
Biochem J. 2010 Apr 28;428(1):113-24. doi: 10.1042/BJ20090867.
4
Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits.非肽类尾加压素 II 受体拮抗剂：基于哌嗪基邻苯二甲酰亚胺和哌嗪基异吲哚啉酮亚基的新型配体类别。
J Med Chem. 2009 Dec 10;52(23):7432-45. doi: 10.1021/jm900683d.
5
Novel and potent small-molecule urotensin II receptor agonists.新型强效小分子尾加压素II受体激动剂。
Bioorg Med Chem. 2009 Jul 1;17(13):4657-65. doi: 10.1016/j.bmc.2009.04.062. Epub 2009 May 3.
6
N-alkyl-5H-pyrido[4,3-b]indol-1-amines and derivatives as novel urotensin-II receptor antagonists.N-烷基-5H-吡啶并[4,3-b]吲哚-1-胺及其衍生物作为新型尾加压素II受体拮抗剂。
Bioorg Med Chem Lett. 2008 Sep 15;18(18):4936-9. doi: 10.1016/j.bmcl.2008.08.054. Epub 2008 Aug 22.
7
Aminomethylpiperazines as selective urotensin antagonists.氨甲基哌嗪作为选择性尿紧张素拮抗剂。
Bioorg Med Chem Lett. 2008 Aug 15;18(16):4470-3. doi: 10.1016/j.bmcl.2008.07.067. Epub 2008 Jul 20.
8
Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues.帕洛苏兰可抑制与细胞膜中灵长类UT受体的结合，但在完整细胞和血管组织中表现出不同的活性。
Br J Pharmacol. 2008 Oct;155(3):374-86. doi: 10.1038/bjp.2008.266. Epub 2008 Jun 30.
9
2-Aminomethyl piperidines as novel urotensin-II receptor antagonists.2-氨甲基哌啶类化合物作为新型尿紧张素II受体拮抗剂
Bioorg Med Chem Lett. 2008 May 1;18(9):2860-4. doi: 10.1016/j.bmcl.2008.03.078. Epub 2008 Apr 8.
10
Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: synthesis, SAR, and in vivo assessment.作为尿紧张素II受体拮抗剂的苯基哌啶-苯并恶嗪酮：合成、构效关系及体内评估
Bioorg Med Chem Lett. 2007 Dec 1;17(23):6489-92. doi: 10.1016/j.bmcl.2007.09.092. Epub 2007 Oct 1.