Laboratory of Blood and Vascular Biology and.
Laboratory of Molecular Electron Microscopy, Rockefeller University, New York, NY.
Blood Adv. 2020 Jul 14;4(13):2939-2949. doi: 10.1182/bloodadvances.2020001545.
Although much is known about the interaction of fibrinogen with αIIbβ3, much less is known about the interaction of platelets with cross-linked fibrin. Fibrinogen residue Lys406 plays a vital role in the interaction of fibrinogen with αIIbβ3, but because it participates in fibrin cross-linking, it is not available for interacting with αIIbβ3. We studied the adhesion of platelets and HEK cells expressing normal and constitutively active αIIbβ3 to both immobilized fibrinogen and D-dimer, a proteolytic fragment of cross-linked fibrin, as well as platelet-mediated clot retraction. Nonactivated platelets and HEK cells expressing normal αIIbβ3 adhered to fibrinogen but not D-dimer, whereas activated platelets as well as HEK cells expressing activated αIIbβ3 both bound to D-dimer. Small-molecule antagonists of the αIIbβ3 RGD (Arg-Gly-Asp) binding pocket inhibited adhesion to D-dimer, and an Asp119Ala mutation that disrupts the β3 metal ion-dependent adhesion site inhibited αIIbβ3-mediated adhesion to D-dimer. D-dimer and a polyclonal antibody against D-dimer inhibited clot retraction. The monoclonal antibody (mAb) 10E5, directed at αIIb and a potent inhibitor of platelet interactions with fibrinogen, did not inhibit the interaction of activated platelets with D-dimer or clot retraction, whereas the mAb 7E3, directed at β3, inhibited both phenomena. We conclude that activated, but not nonactivated, αIIbβ3 mediates interactions between platelets and D-dimer, and by extrapolation, to cross-linked fibrin. Although the interaction of αIIbβ3 with D-dimer differs from that with fibrinogen, it probably involves contributions from regions on β3 that are close to, or that are affected by, changes in the RGD binding pocket.
虽然人们对纤维蛋白原与αIIbβ3 的相互作用了解很多,但对血小板与交联纤维蛋白的相互作用知之甚少。纤维蛋白原残基 Lys406 在纤维蛋白原与αIIbβ3 的相互作用中起着至关重要的作用,但由于它参与了纤维蛋白的交联,因此无法与αIIbβ3 相互作用。我们研究了正常和组成型激活的αIIbβ3 表达的血小板和 HEK 细胞与固定化纤维蛋白原和 D-二聚体(交联纤维蛋白的蛋白水解片段)的粘附,以及血小板介导的凝块回缩。非激活的血小板和表达正常αIIbβ3 的 HEK 细胞粘附于纤维蛋白原,但不粘附于 D-二聚体,而激活的血小板和表达激活的αIIbβ3 的 HEK 细胞均与 D-二聚体结合。αIIbβ3 的 RGD(精氨酸-甘氨酸-天冬氨酸)结合口袋的小分子拮抗剂抑制了与 D-二聚体的粘附,破坏β3 金属离子依赖性粘附位点的 Asp119Ala 突变抑制了αIIbβ3 介导的与 D-二聚体的粘附。D-二聚体和针对 D-二聚体的多克隆抗体抑制了凝块回缩。针对αIIb 的单克隆抗体(mAb)10E5 是一种强效的血小板与纤维蛋白原相互作用抑制剂,它不抑制激活的血小板与 D-二聚体的相互作用或凝块回缩,而针对β3 的 mAb 7E3 则抑制这两种现象。我们得出结论,激活的而非非激活的αIIbβ3 介导血小板与 D-二聚体之间的相互作用,并推断交联纤维蛋白也是如此。尽管αIIbβ3 与 D-二聚体的相互作用与纤维蛋白原不同,但它可能涉及到β3 上靠近或受 RGD 结合口袋变化影响的区域的贡献。