STAUROSPORINE, A POTENT INHIBITOR OF PHOSPHOLIPID/CA++DEPENDENT PROTEIN-KINASE
STAUROSPORINE, A POTENT INHIBITOR OF PHOSPHOLIPID/CA++DEPENDENT PROTEIN-KINASE
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DOI：
10.1016/0006-291x(86)90008-2
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发表时间：
1986-03-13
影响因子：
3.1
通讯作者：
TOMITA, F
中科院分区：
文献类型：
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作者：
TAMAOKI, T;NOMOTO, H;TOMITA, F
已知具有抗真菌活性的微生物生物碱Staurosporine被发现显著抑制来自大鼠脑的磷脂/Ca 2+依赖性蛋白激酶（蛋白激酶C），IC 50值为2.7 nM。但对3 H-佛波醇-12，13-二丁酸酯（PDBu）与蛋白激酶C的结合无明显影响。对蛋白激酶C的抑制作用与磷脂无竞争性。该化合物对HeLa S3细胞的生长也显示出强的细胞毒性作用，其IC 50值为4 × 104。10-12 M。
Staurosporine, microbial alkaloid which has been known to have antifungal activity was found to inhibit markedly phospholipid/Ca2+ dependent protein kinase (protein kinase C) from rat brain, with an IC50 value of 2.7 nM. However, it had little effect on the binding of 3H-phorbol-12,13-dibutyrate (PDBu) to protein kinase C. The inhbition of protein kinase C was not competitive with phospholipid. This compound also showed the strong cytotoxic effect on the growth of HeLa S3 cells, with an IC50 value of 4 .times. 10-12 M under the condition of 72 hr-exposure.