The main role of platelets is to contribute to hemostasis. However, under pathophysiological conditions, platelet activation may lead to thrombotic events of cardiovascular diseases. Thus, anti-thrombotic treatment is important in patients with cardiovascular disease. This review focuses on a platelet receptor, a transmembrane protein, the Multidrug Resistance Protein 4, MRP4, which contributes to platelet activation, by extruding endogenous molecules responsible for their activation and accumulation. The regulation of the intracellular concentration levels of these molecules by MRP4 turned to make the protein suspicious and at the same time an interesting regulatory factor of platelet normal function. Especially, the possible role of MRP4 in the excretion of xenobiotic and antiplatelet drugs such as aspirin is discussed, thus imparting platelet aspirin tolerance and correlating the protein with the ineffectiveness of aspirin antiplatelet therapy. Based on the above, this review finally underlines that the development of a highly selective and targeted strategy for platelet MRP4 inhibition will also lead to inhibition of platelet activation and accumulation.

血小板的主要作用是有助于止血。然而，在病理生理条件下，血小板活化可能导致心血管疾病的血栓事件。因此，抗血栓治疗对于心血管疾病患者很重要。本综述重点关注血小板受体，一种跨膜蛋白，多药耐药蛋白 4，MRP4，它通过挤压负责血小板活化和积累的内源性分子来促进血小板活化。MRP4 对这些分子的细胞内浓度水平的调节使蛋白质变得可疑，同时也是血小板正常功能的有趣调节因子。特别讨论了 MRP4 在异生物质和抗血小板药物（如阿司匹林）排泄中的可能作用，因此赋予血小板阿司匹林耐受性并将蛋白质与阿司匹林抗血小板治疗的无效联系起来。基于上述，本综述最后强调，开发一种高选择性和靶向的血小板 MRP4 抑制策略也将导致血小板活化和积聚的抑制。