SURAMIN, AN ANTI-CANCER DRUG, INHIBITS PROTEIN KINASE-C AND INDUCES DIFFERENTIATION IN NEURO-BLASTOMA CELL CLONE NB2A
SURAMIN, AN ANTI-CANCER DRUG, INHIBITS PROTEIN KINASE-C AND INDUCES DIFFERENTIATION IN NEURO-BLASTOMA CELL CLONE NB2A
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DOI：
10.1016/0014-5793(89)81639-4
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发表时间：
1989-11-20
期刊：
影响因子：
3.5
通讯作者：
AZZI, A
中科院分区：
文献类型：
--
作者：
HENSEY, CE;BOSCOBOINIK, D;AZZI, A
从大鼠脑中纯化的蛋白激酶C被苏拉明抑制，苏拉明是一种最初用于抗锥虫感染治疗的物质，最近被提议作为抗锥虫剂。苏拉明对酶的抑制作用与底物之一ATP呈竞争性，其aKi为10 μM。在足以抑制分离的酶的浓度下，苏拉明显示出在体外减缓神经母细胞瘤NB2A细胞的增殖速率，并诱导其分化，如典型的形态学变化所证明的。
Protein kinase C purified from rat brain was found to be inhibited by suramin, a substance used originally in the therapy of antitrypanosomic infections and more recently proposed as antineoplastic agent. The inhibition of suramin was competitive with one of the substrates of the enzyme, ATP with aKiof 10 μM. At concentrations adequate to inhibit the isolated enzyme, suramin was shown to slow the rate of proliferation of neuroblastoma NB2A cells in vitro and to induce their differentiation as evidenced by typical morphological changes.