Advantages of fast-acting ADP receptor blockade in ischemic heart disease.
Advantages of fast-acting ADP receptor blockade in ischemic heart disease.
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速效 ADP 受体阻断在缺血性心脏病中的优势。
DOI：
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发表时间：
2003
期刊：
影响因子：
--
通讯作者：
P. Nurden
中科院分区：
文献类型：
--
作者：
A. Nurden;P. Nurden
近年来，ADP在血小板聚集中的刺激作用受到了广泛关注。1 ADP不仅本身是一种主要的生理激动剂，它还在通过其他刺激物（胶原蛋白和肾上腺素是很好的例子）促进聚集中发挥关键作用。ADP从受损组织和血细胞释放，包括分泌血小板，是冠状动脉疾病的主要因素，有利于血小板在狭窄和破裂的动脉粥样硬化斑块部位积聚。最近的进展已经确定了ADP如何在涉及两种受体P2Y1和P2Y12的过程中激活血小板，这两种受体都属于G蛋白偶联的七跨膜结构域受体家族。P2Y12是先天性缺陷的患者的发现2，3和最近克隆的P2Y12已被证明是一个最难以捉摸的受体，推进了研究。根据目前的想法，血小板与P2Y1的相互作用导致形状变化，钙动员，和快速可逆的聚集。与P2Y12的同时结合允许形成大的、稳定的血小板聚集体。似乎P2Y1开始聚合，然后P2Y12接管。P2Y12的这种作用在其克隆之前就已经被推测出来，当时作为神秘的“P2T”，它已经被认为是抗血栓治疗的主要靶点。现已证实，P2Y12是长效抗血栓药物氯吡格雷和噻氯匹定的作用部位，广泛用于下调冠状动脉疾病中的血小板反应性。6第三种据称的ADP血小板受体，即离子通道P2X1，目前已知主要与ATP反应。
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The stimulatory role of ADP in platelet aggregation has received much attention in recent years.1 Not only is ADP a major physiological agonist on its own, it also plays a key role in promoting aggregation by other stimuli of which collagen and epinephrine are excellent examples. Released from damaged tissues and blood cells, including secreting platelets, ADP is a major factor in coronary artery disease favoring platelet accumulation at sites of stenosis and fissured atherosclerotic plaques. Recent advances have defined how ADP activates platelets in a process involving two receptors, P2Y1 and P2Y12, both belonging to the G-protein–coupled seven-transmembrane domain receptor family. Studies were advanced by the discovery of patients in which P2Y12 is congenitally deficient2,3⇓ and by the recent cloning of P2Y12 which had proved a most elusive receptor.2–5⇓⇓⇓ According to current thinking, interaction of platelets with P2Y1 leads to shape change, calcium mobilization, and a rapidly reversible aggregation. Simultaneous binding to P2Y12 permits the formation of large, stable platelet aggregates. It appears that P2Y1 starts the aggregation, and then P2Y12 takes over. This role of P2Y12 had been speculated on before its cloning when, as the mysterious “P2T,” it was already considered to be a primary target for antithrombotic therapy. It has now been confirmed that P2Y12 is the site of action of the long-acting antithrombotic drugs clopidogrel and ticlopidine, widely used to downregulate platelet reactivity in coronary artery disease.6 A third purported platelet receptor for ADP, the ion channel P2X1, is now known to react primarily with ATP.
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需要阻断二磷酸腺苷受体 P2Y(12) 和 P2Y(1) 才能抑制流动下全血中的血小板聚集。
影响因子：
20.3
作者：
Turner,NA;Moake,JL;McIntire,LV
通讯作者：
McIntire,LV
影响因子：
15.9
作者：
Marcus, AJ;Broekman, MJ;Maliszewski, CR
通讯作者：
Maliszewski, CR
二磷酸腺苷诱导冯维勒布兰德因子与人血小板的结合。
影响因子：
64.8
作者：
Fujimoto,T;Hawiger,J
通讯作者：
Hawiger,J
对接受氯吡格雷的人类受试者和患有 ADP 依赖性血小板活化途径遗传缺陷的患者的血小板聚集体进行超微结构研究。
DOI：
10.1161/01.atv.16.12.1532
发表时间：
1996
期刊：
Arteriosclerosis, thrombosis, and vascular biology
影响因子：
--
作者：
Humbert,M;Nurden,P;Bihour,C;Pasquet,JM;Winckler,J;Heilmann,E;Savi,P;Herbert,JM;Kunicki,TJ;Nurden,AT
通讯作者：
Nurden,AT