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。