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血小板活化时,表面GPⅡb/Ⅲa受体变构,与纤维蛋白结合形成血栓.纤维蛋白识别GPⅡb/Ⅲa受体时,RGD(Arg-Gly-Asp)是关键序列.含RGD多肽可以竞争GPⅡb/Ⅲa受体,进而阻断血栓形成进程.作者注意到,含RGD多肽的抗血栓活性与构象关系密切.采用Biosym公司设计的Discover程序,计算了RGDS(Arg-Gly-Asp-Ser),RGDV(Arg-Gly-Asp-Val)和RGDF(Arg-Gly-Asp-Phe)在真空下、在水中和在正辛醇中的右手螺旋、左手螺旋及β伸展构象,讨论了构象对抗血栓活性的影响
Platelet activation, the surface of GP Ⅱ b / Ⅲ a receptor allosteric, fibrin and thrombosis. RGD (Arg-Gly-Asp) is the key sequence when fibrin recognizes GPⅡb / Ⅲa receptor. RGD-containing peptides can compete with GPIIb / IIIa receptors, thereby blocking the thrombosis process. The authors note that the antithrombotic activity of RGD-containing peptides is closely related to the conformation. RGDS (Arg-Gly-Asp-Ser), RGDV (Arg-Gly-Asp-Val) and RGDF (Arg-Gly-Asp-Phe) were calculated under vacuum in water using a Discover program designed by Biosym, Right-handed helix, left-handed helix, and beta-extension conformation in n-octanol, the effect of conformation on antithrombotic activity was discussed