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活化的血小板暴露膜糖蛋白复合物(GPⅡb/Ⅲa),作为受体识别结合纤维蛋白原(Pg)等粘附蛋白共有的精氨酰─甘氨酰─天冬氨酸(Arg-Gly-Asp,即RGD)序列,导致血小板聚集和血栓形成。人工合成的含RGD多肽可阻断GPⅡb/Ⅲa与Fg等结合,从而抑制血小板聚集和血栓形成。为了开展肽类血小板聚集抑制剂的研究,我们用液相法合成了Ac-Arg-Gly一Asp-NHCH2CH2Ph。初步体外活性实验结果表明,该RGD肽衍生物对ADP诱导的血小板聚集具有较强的抑制作用,在血浆中3h作用强度基本不变。
Activated platelet-exposed membrane glycoprotein complex (GP IIb / IIIa) as a receptor for recognition of arginine-glycyl-aspartate (Arg-Gly-Asp) common to adhesion proteins such as fibrinogen (Pg) , The RGD) sequence, leading to platelet aggregation and thrombosis. Synthetic RGD-containing peptides can block GP Ⅱ b / Ⅲ a and Fg and other binding, thereby inhibiting platelet aggregation and thrombosis. In order to carry out the study of peptide platelet aggregation inhibitors, we synthesized Ac-Arg-Gly-Asp-NHCH2CH2Ph by liquid-phase method. The results of preliminary in vitro experiments showed that the derivatives of RGD peptide had a strong inhibitory effect on platelet aggregation induced by ADP, and remained unchanged in plasma at 3h.