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作 者:朱奕霖 彭婕 施小凤 Zhu Yilin;Peng Jie;Shi Xiaofeng(Department of Hematology,Affiliated Hospital of Jiangsu University,Zhenjiang 212001,Jiangsu Province,China;Department of Hematology,Second Affiliated Hospital of Nanjing Medical University,Nanjing 210000,Jiangsu Province,China)
机构地区:[1]江苏大学附属医院血液科,镇江202001 [2]南京医科大学第二附属医院血液科,南京210000
出 处:《国际输血及血液学杂志》2023年第1期26-33,共8页International Journal of Blood Transfusion and Hematology
基 金:国家自然科学基金(81700130);镇江市科技创新资金(SH2017006)。
摘 要:近年,心脑血管血栓性疾病的发生率逐年增高,而引起血栓性疾病的首要原因是病理性血栓的形成。血小板在止血和血栓形成中发挥重要作用。整合素αⅡbβ3是血小板表面表达最丰富的受体,且是血小板活化聚集的终末通路。整合素αⅡbβ3拮抗剂,如阿昔单抗、依替巴肽及替罗非班,具有抑制血栓形成作用,但其在抗血栓的同时可导致严重出血,因此如何在抗血栓的同时降低出血发生率是相关研究热点。整合素αⅡbβ3可介导血小板双向信号转导,因此研发新型拮抗剂,选择性地阻断细胞外向细胞内信号转导而不影响细胞内向细胞外信号转导,可发挥抗血栓作用而不导致出血,是新的抗血栓策略。笔者拟重点对整合素αⅡbβ3及其在血小板相关信号通路中的作用,以及各种靶向整合素αⅡbβ3的抗血栓药物进行介绍,为临床抗血栓治疗提供新思路。In recent years,incidence of cardiovascular and cerebrovascular thrombotic diseases has increased gradually.The primary cause of thrombotic diseases is the formation of pathological thrombosis.Platelets play an important role in hemostasis and thrombosis.IntegrinαⅡbβ3 is the most abundant receptor on platelet surface,and is the terminal common pathway of platelet activation.Antagonists of integrinαⅡbβ3,such as abciximab,eptifiatide and tirofiban,can inhibit thrombus formation effectively,but at same time can cause serious adverse effect of bleeding.How to inhibit the thrombus formation but to reduce the incidence of bleeding is a relevant research hotspot.IntegrinαⅡbβ3 mediates platelet bidirectional signal transduction.Selective inhibition of outside-in signal transduction without affecting inside-out signal transduction by novel antagonists is a new antithrombotic strategy.This paper intends to focus on integrinαⅡbβ3,and its role in platelet related signal transduction,and various antithrombotic drugs targeting integrinαⅡbβ3,to provide a new idea for clinical antithrombotic therapy.
关 键 词:血小板 整合素类 血栓形成 止血 整合素αⅡbβ3 拮抗剂
分 类 号:R54[医药卫生—心血管疾病]
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