Rodríguez-Liñares B, Watson S P
Department of Pharmacology, University of Oxford, U.K.
Biochem J. 1996 May 15;316 ( Pt 1)(Pt 1):93-8. doi: 10.1042/bj3160093.
Thrombopoietin (TPO), also known as the c-mpl ligand, stimulates rapid tyrosine phosphorylation of multiple proteins in human platelets including the Janus family kinases JAK2 and TYK2. On its own, TPO has no effect on platelet aggregation and dense-granule secretion but induces a general potentiation of these responses by other stimuli. The most dramatic effect is observed against threshold concentrations of agonists for aggregation. Shape change or weak reversible aggregation induced by low concentrations of thrombin, collagen and the thromboxane mimetic, U46619, are converted into irreversible aggregation in the presence of TPO. A similar result is obtained in the presence of the ADP scavenger apyrase and cyclo-oxygenase inhibitor indomethacin. TPO also induces potentiation of dense-granule secretion measured through release of 5-hydroxy[3H]-tryptamine. This effect is most striking against low concentrations of stimuli and is independent of aggregation as it is observed in the presence of chelation of extracellular Ca2+ with EGTA. TPO potentiates activation of phospholipase C and elevation of intracellular Ca2+, providing a molecular explanation for potentiation of functional responses. TPO may have an important physiological role in priming platelet activation in thrombocytopenia, an action that may help to compensate for the reduced platelet density.
血小板生成素(TPO),也被称为c-mpl配体,可刺激人血小板中多种蛋白质的快速酪氨酸磷酸化,包括Janus家族激酶JAK2和TYK2。TPO本身对血小板聚集和致密颗粒分泌没有影响,但可增强其他刺激引发的这些反应。在针对聚集的激动剂阈值浓度时可观察到最显著的效果。低浓度凝血酶、胶原蛋白和血栓素类似物U46619诱导的形态改变或弱可逆聚集,在TPO存在时会转变为不可逆聚集。在存在ADP清除剂腺苷三磷酸双磷酸酶和环氧化酶抑制剂吲哚美辛的情况下也可获得类似结果。TPO还可增强通过5-羟色胺[³H]释放来测定的致密颗粒分泌。这种作用在针对低浓度刺激时最为显著,且与聚集无关,因为在存在用乙二醇双四乙酸螯合细胞外Ca²⁺的情况下也可观察到。TPO增强磷脂酶C的激活和细胞内Ca²⁺的升高,为功能反应的增强提供了分子解释。TPO在血小板减少症中启动血小板激活方面可能具有重要的生理作用,这一作用可能有助于补偿降低的血小板密度。