• 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

蛋白酶受体拮抗作用靶向血小板治疗。

Protease receptor antagonism to target blood platelet therapies.

机构信息

University of Michigan Medical School, Departments of Pharmacology and Internal Medicine, Ann Arbor, Michigan, USA.

Thomas Jefferson University, The Cardeza Foundation for Hematologic Research and the Department of Medicine, Jefferson Medical College, Philadelphia, Pennsylvania, USA.

出版信息

Clin Pharmacol Ther. 2016 Jan;99(1):72-81. doi: 10.1002/cpt.282. Epub 2015 Nov 18.

DOI:10.1002/cpt.282
PMID:26501993
Abstract

Platelet activation and thrombus formation play a central role in ischemic vascular disease. Thrombin, an especially potent physiologic agonist mediating in vivo activation of platelets, acts via a unique family of G-protein-coupled receptors called protease-activated receptors (PARs) with a broad tissue expression. This review focuses on current antiplatelet therapies as well as innovative approaches to targeting PARs in patients with atherothrombotic vascular disease.

摘要

血小板激活和血栓形成在缺血性血管疾病中起着核心作用。凝血酶是一种特别有效的生理激动剂,可介导血小板的体内激活,它通过一种独特的称为蛋白酶激活受体 (PARs) 的 G 蛋白偶联受体家族发挥作用,具有广泛的组织表达。本文重点介绍了目前的抗血小板治疗方法,以及针对动脉血栓形成性血管疾病患者的 PAR 靶向创新方法。

相似文献

1
Protease receptor antagonism to target blood platelet therapies.蛋白酶受体拮抗作用靶向血小板治疗。
Clin Pharmacol Ther. 2016 Jan;99(1):72-81. doi: 10.1002/cpt.282. Epub 2015 Nov 18.
2
Platelet thrombin receptor antagonism with vorapaxar: pharmacology and clinical trial development.沃拉帕沙对血小板凝血酶受体的拮抗作用:药理学与临床试验进展
Future Cardiol. 2015 Sep;11(5):547-64. doi: 10.2217/fca.15.50. Epub 2015 Sep 25.
3
G-protein-coupled receptors as signaling targets for antiplatelet therapy.作为抗血小板治疗信号靶点的G蛋白偶联受体
Arterioscler Thromb Vasc Biol. 2009 Apr;29(4):449-57. doi: 10.1161/ATVBAHA.108.176388. Epub 2008 Nov 20.
4
Using PAR4 Inhibition as an Anti-Thrombotic Approach: Why, How, and When?使用 PAR4 抑制作为抗血栓形成的方法:为什么、如何以及何时?
Int J Mol Sci. 2019 Nov 11;20(22):5629. doi: 10.3390/ijms20225629.
5
Selective inhibition of protease-activated receptor 4-dependent platelet activation by YD-3.YD-3对蛋白酶激活受体4依赖性血小板活化的选择性抑制作用
Thromb Haemost. 2002 Jun;87(6):1026-33.
6
Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding.阻断蛋白酶激活受体 4(PAR4)可提供强大的抗血栓活性,同时出血风险低。
Sci Transl Med. 2017 Jan 4;9(371). doi: 10.1126/scitranslmed.aaf5294.
7
Inhibitors of the platelet thrombin receptor: will they live up to their promises?血小板凝血酶受体抑制剂:它们会不负所望吗?
Circulation. 2011 May 3;123(17):1833-5. doi: 10.1161/CIRCULATIONAHA.111.021733. Epub 2011 Apr 18.
8
Protease-Activated Receptor 4 (PAR4): A Promising Target for Antiplatelet Therapy.蛋白酶激活受体 4(PAR4):抗血小板治疗的有前途靶点。
Int J Mol Sci. 2018 Feb 14;19(2):573. doi: 10.3390/ijms19020573.
9
Platelet protease-activated receptor antagonism in cardiovascular medicine.心血管医学中的血小板蛋白酶激活受体拮抗作用。
Coron Artery Dis. 2012 Sep;23(6):375-9. doi: 10.1097/MCA.0b013e3283564946.
10
Physiology, pharmacology, and therapeutic potential of protease-activated receptors in vascular disease.血管疾病中蛋白酶激活受体的生理学、药理学和治疗潜力。
Pharmacol Ther. 2012 May;134(2):246-59. doi: 10.1016/j.pharmthera.2012.01.007. Epub 2012 Jan 30.

引用本文的文献

1
Generalized Michaelis-Menten rate law with time-varying molecular concentrations.具有时变分子浓度的广义米氏酶动力学定律。
PLoS Comput Biol. 2023 Dec 11;19(12):e1011711. doi: 10.1371/journal.pcbi.1011711. eCollection 2023 Dec.
2
The predominant PAR4 variant in individuals of African ancestry worsens murine and human stroke outcomes.非洲裔个体中主要的 PAR4 变体可使鼠类和人类的中风预后恶化。
J Clin Invest. 2023 Sep 15;133(18):e169608. doi: 10.1172/JCI169608.
3
Neutrophil cathepsin G proteolysis of protease-activated receptor 4 generates a novel, functional tethered ligand.
中性粒细胞组织蛋白酶 G 对蛋白酶激活受体 4 的蛋白水解作用产生了一种新型的、有功能的连接配体。
Blood Adv. 2022 Apr 12;6(7):2303-2308. doi: 10.1182/bloodadvances.2021006133.
4
The protease-activated receptor 4 Ala120Thr variant alters platelet responsiveness to low-dose thrombin and protease-activated receptor 4 desensitization, and is blocked by non-competitive P2Y inhibition.蛋白酶激活受体 4 第 120 位的丙氨酸突变为苏氨酸变异体改变了血小板对低剂量凝血酶和蛋白酶激活受体 4 脱敏的反应性,并且被非竞争性 P2Y 抑制所阻断。
J Thromb Haemost. 2018 Dec;16(12):2501-2514. doi: 10.1111/jth.14318. Epub 2018 Nov 22.
5
Humanizing the Protease-Activated Receptor (PAR) Expression Profile in Mouse Platelets by Knocking PAR1 into the Par3 Locus Reveals PAR1 Expression Is Not Tolerated in Mouse Platelets.通过将PAR1敲入Par3基因座使小鼠血小板中的蛋白酶激活受体(PAR)表达谱人源化,揭示了PAR1在小鼠血小板中不能被耐受。
PLoS One. 2016 Oct 27;11(10):e0165565. doi: 10.1371/journal.pone.0165565. eCollection 2016.