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蛋白激酶抑制剂星形孢菌素不抑制磷酸肌醇激酶。

The protein kinase inhibitor, staurosporine, does not inhibit phosphoinositide kinases.

作者信息

Smith C D, Mooberry S L

机构信息

Cancer Research Center of Hawaii, University of Hawaii, Honolulu 96813.

出版信息

Biochem Int. 1992 Mar;26(4):679-85.

PMID:1319150
Abstract

The effects of the protein kinase inhibitor staurosporine on phosphatidylinositol (PI) kinase and phosphatidylinositol 4-phosphate (PIP) kinase activities in brain membranes, and the synthesis of polyphosphoinositides in cultured NIH 3T3 fibroblasts were examined. Staurosporine, at concentrations up to 1 microM did not significantly modulate either PI kinase or PIP kinase activity in brain membranes. DNA synthesis was dose-dependently inhibited by sub-nanomolar concentrations of staurosporine; however, cells treated with up to 1 microM staurosporine contained levels of PIP and phosphatidylinositol 4,5-bisphosphate (PIP2) similar to those observed in untreated cells. Therefore, phosphoinositide kinases do not appear to be either directly or indirectly affected by staurosporine.

摘要

研究了蛋白激酶抑制剂星形孢菌素对脑膜中磷脂酰肌醇(PI)激酶和磷脂酰肌醇4-磷酸(PIP)激酶活性的影响,以及对培养的NIH 3T3成纤维细胞中多磷酸肌醇合成的影响。浓度高达1微摩尔的星形孢菌素对脑膜中的PI激酶或PIP激酶活性均无显著调节作用。亚纳摩尔浓度的星形孢菌素可剂量依赖性地抑制DNA合成;然而,用高达1微摩尔星形孢菌素处理的细胞中PIP和磷脂酰肌醇4,5-二磷酸(PIP2)的水平与未处理细胞中观察到的水平相似。因此,磷酸肌醇激酶似乎未受到星形孢菌素的直接或间接影响。

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