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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.
2
Identification of the minimum PAR4 inhibitor pharmacophore and optimization of a series of 2-methoxy-6-arylimidazo[2,1-b][1,3,4]thiadiazoles.最小PAR4抑制剂药效团的鉴定及一系列2-甲氧基-6-芳基咪唑并[2,1-b][1,3,4]噻二唑的优化。
Bioorg Med Chem Lett. 2016 Nov 15;26(22):5481-5486. doi: 10.1016/j.bmcl.2016.10.020. Epub 2016 Oct 11.
3
Platelet clearance via shear-induced unfolding of a membrane mechanoreceptor.通过膜机械感受器的剪切诱导展开实现血小板清除
Nat Commun. 2016 Sep 27;7:12863. doi: 10.1038/ncomms12863.
4
Identification of a juxtamembrane mechanosensitive domain in the platelet mechanosensor glycoprotein Ib-IX complex.血小板机械传感器糖蛋白Ib-IX复合物中近膜机械敏感结构域的鉴定。
Blood. 2015 Jan 15;125(3):562-9. doi: 10.1182/blood-2014-07-589507. Epub 2014 Oct 30.
5
Biased signaling of protease-activated receptors.蛋白酶激活受体的偏向性信号传导
Front Endocrinol (Lausanne). 2014 May 13;5:67. doi: 10.3389/fendo.2014.00067. eCollection 2014.
6
Differential signaling by protease-activated receptors: implications for therapeutic targeting.蛋白酶激活受体的差异信号传导:对治疗靶点的影响。
Int J Mol Sci. 2014 Apr 11;15(4):6169-83. doi: 10.3390/ijms15046169.
7
Synthesis of indole derived protease-activated receptor 4 antagonists and characterization in human platelets.吲哚衍生蛋白酶激活受体 4 拮抗剂的合成及其在人血小板中的特征。
PLoS One. 2013 Jun 11;8(6):e65528. doi: 10.1371/journal.pone.0065528. Print 2013.
8
Clinical Pharmacogenetics Implementation Consortium guidelines for CYP2C19 genotype and clopidogrel therapy: 2013 update.临床药物遗传学实施联盟 CYP2C19 基因型和氯吡格雷治疗指南:2013 年更新。
Clin Pharmacol Ther. 2013 Sep;94(3):317-23. doi: 10.1038/clpt.2013.105. Epub 2013 May 22.
9
Protease-activated receptor (PAR) 1 and PAR4 differentially regulate factor V expression from human platelets.蛋白酶激活受体(PAR)1 和 PAR4 可调节人血小板中因子 V 的表达。
Mol Pharmacol. 2013 Apr;83(4):781-92. doi: 10.1124/mol.112.083477. Epub 2013 Jan 10.
10
New fundamentals in hemostasis.止血的新基础。
Physiol Rev. 2013 Jan;93(1):327-58. doi: 10.1152/physrev.00016.2011.

Protease activated receptor 4: a backup receptor or a dark horse as a target in antiplatelet therapy?

作者信息

Han Xu, Nieman Marvin T

机构信息

Department of Pharmacology, Case Western Reserve University, Cleveland, OH, USA.

出版信息

Ann Transl Med. 2018 Feb;6(3):56. doi: 10.21037/atm.2017.11.36.

DOI:10.21037/atm.2017.11.36
PMID:29610748
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5879510/
Abstract
摘要