K-252a：神经生长因子对PC12细胞作用的特异性抑制剂。
K-252a: a specific inhibitor of the action of nerve growth factor on PC 12 cells.
作者信息
Koizumi S, Contreras M L, Matsuda Y, Hama T, Lazarovici P, Guroff G
机构信息
Section on Growth Factors, National Institutes of Child Health and Human Development, Bethesda, Maryland 20892.
出版信息
J Neurosci. 1988 Feb;8(2):715-21. doi: 10.1523/JNEUROSCI.08-02-00715.1988.
K-252a, a kinase inhibitor isolated from the culture broth of Nocardiopsis sp., selectively inhibits the actions of nerve growth factor (NGF) on PC 12 cells. At a concentration of 200 nM, K-252a prevents neurite generation initiated by NGF, but not neurite generation produced by fibroblast growth factor or outgrowth produced by dibutyryl cAMP. K-252a also inhibits the induction of ornithine decarboxylase by NGF, but stimulates ornithine decarboxylase induction by epidermal growth factor. Stimulation of phosphatidylinositol breakdown by NGF was similarly inhibited by K-252a, while stimulation by epidermal growth factor was enhanced. The NGF-induced decrease in the phosphorylation of a soluble protein, Nsp 100, was prevented by K-252a. K-252a blocks the NGF-induced heterodown-regulation of the epidermal growth factor receptor, but not the epidermal growth factor-induced homodown-regulation of the epidermal growth factor receptor. K-252a, then, provides a new tool for the dissection and study of NGF-requiring processes.
K-252a是一种从诺卡氏菌属菌种的培养液中分离出的激酶抑制剂，它能选择性抑制神经生长因子（NGF）对PC12细胞的作用。在浓度为200 nM时，K-252a可阻止由NGF引发的神经突生成，但不会阻止成纤维细胞生长因子产生的神经突生成或二丁酰环磷腺苷产生的神经突生长。K-252a还能抑制NGF诱导的鸟氨酸脱羧酶，但能刺激表皮生长因子诱导的鸟氨酸脱羧酶。K-252a同样能抑制NGF对磷脂酰肌醇分解的刺激作用，而对表皮生长因子的刺激作用则有增强。K-252a可阻止NGF诱导的可溶性蛋白Nsp 100磷酸化减少。K-252a能阻断NGF诱导的表皮生长因子受体异源下调，但不能阻断表皮生长因子诱导的表皮生长因子受体同源下调。因此，K-252a为剖析和研究需要NGF的过程提供了一种新工具。
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