首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Effects of prodigiosin family compounds from Pseudoalteromonas sp. 1020R on the activities of protein phosphatases and protein kinases
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Effects of prodigiosin family compounds from Pseudoalteromonas sp. 1020R on the activities of protein phosphatases and protein kinases

机译:假单孢菌属prodigiosin家族化合物的影响。 1020R对蛋白磷酸酶和蛋白激酶活性的影响

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Pseudoalteromonas sp. strain 1020R produces prodigiosin and its closely related congeners, which differ in the length of their alkyl side chains. These red-pigmented compounds were found to exhibit cytotoxicity against human leukemia cell lines. The compounds also showed dose-dependent inhibitory effects on protein phosphatase 2A and protein tyrosine phosphatase 1B (PTP1B), while remaining relatively inactive against protein kinases, including protein tyrosine kinase, Ca2+/calmodulin-dependent protein kinase and protein kinases A and C. Comparative studies of the individual pigmented compounds on PTP1B inhibition showed that as the chain length of the alkyl group at the C-3 position of the compound increased, the inhibitory effect on PTP1B decreased. These results suggest that protein phosphatases but not protein kinases might be involved in the cytotoxicity of the prodigiosin family of compounds against malignant cells.
机译:假单胞菌菌株1020R产生prodigiosin及其密切相关的同类物,它们的烷基侧链长度不同。发现这些红色色素的化合物对人白血病细胞系表现出细胞毒性。这些化合物还对蛋白磷酸酶2A和酪氨酸磷酸酶1B(PTP1B)表现出剂量依赖性抑制作用,而对蛋白激酶(包括蛋白酪氨酸激酶,Ca 2 + /钙调蛋白依赖性蛋白)保持相对无活性。每种色素化合物对PTP1B抑制的比较研究表明,随着化合物C-3位烷基的链长增加,对PTP1B的抑制作用降低。这些结果表明,蛋白磷酸酶而不是蛋白激酶可能参与了prodigiosin家族的化合物对恶性细胞的细胞毒性。

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