BRYOSTATINS MIMIC THE EFFECTS OF PHORBOL ESTERS IN INTACT HUMAN-PLATELETS
BRYOSTATINS MIMIC THE EFFECTS OF PHORBOL ESTERS IN INTACT HUMAN-PLATELETS
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DOI：
10.1016/0167-4889(87)90239-4
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发表时间：
1987-06-15
期刊：
影响因子：
--
通讯作者：
WALLACE, RW
中科院分区：
文献类型：
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作者：
TALLANT, EA;SMITH, JB;WALLACE, RW
苔藓抑素-7诱导人血小板的聚集和特异性血小板蛋白的磷酸化。聚集的速率和程度与肿瘤促进剂佛波酯12-肉豆蔻酸酯13-乙酸酯（PMA）诱导的相似;然而，与凝血酶诱导的反应速率相比，反应速率显著降低。苔藓抑素-7到32 P标记的血小板的添加导致32 P到20，47和250 kDa的蛋白质中的时间依赖性掺入;响应于凝血酶或PMA的添加，类似分子量的蛋白质被磷酸化。byrostatin-7诱导的磷酸化的时间过程和剂量反应与PMA相似。此外，苔藓抑素-7增加了32 P掺入血小板多磷酸肌醇的水平，这也发生在对PMA的反应中。这些结果表明，在完整的人血小板中，苔藓抑素-7通过直接激活蛋白激酶C模拟佛波酯肿瘤促进剂。
Bryostatin-7 induces aggregation of human platelets and the phosphorylation of specific platelet proteins. Both the rate and extent of aggregation are similar to that induced by the tumor promoter phorbol ester 12-myristate 13-acetate (PMA); however, the rate of response is markedly reduced compared to that induced by thrombin. The addition of bryostatin-7 to 32P-labeled platelets results in a time-dependent incorporation of 32P into proteins of 20, 47 and 250 kDa; proteins of similar molecular mass are phosphorylated in response to the addition of thrombin or PMA. The time courses and doses responses of the phosphorylations induced by byrostatin-7 are similar to those found with PMA. In addition, bryostatin-7 increases the level of 32P incorporation into platelet polyphosphoinositides, which also occurs in response to PMA. These results suggest that, in intact human platelets, bryostatin-7 mimics the phorbol ester tumor promoter by directly activating protein kinase C.