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H-7可降低[3H]地塞米松在大鼠肝切片中的核结合,但不影响糖皮质激素受体的磷酸化。

H-7 reduces the nuclear binding of [3H]dexamethasone in rat liver slices but does not affect the phosphorylation of glucocorticoid receptor.

作者信息

Sharma R, Kido H, Katunuma N

机构信息

Division of Enzyme Chemistry, University of Tokushima, Japan.

出版信息

Biochem Med Metab Biol. 1991 Oct;46(2):246-54. doi: 10.1016/0885-4505(91)90072-s.

Abstract

The effect of 1-(5-isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride (H-7), an inhibitor of protein kinase C, on the nuclear binding of [3H]dexamethasone and on the phosphorylation of glucocorticoid receptor was studied in rat liver slices to ascertain the role of protein kinase C in the expression of glucocorticoid action. H-7 reduces the nuclear binding of [3H]dexamethasone in rat liver slices. It does not affect the extent of phosphorylation of glucocorticoid receptor both in the absence or in the presence of glucocorticoid. These findings indicate that protein kinase C may be involved in the nuclear binding of glucocorticoid receptor but does not directly influence the receptor phosphorylation.

摘要

研究了蛋白激酶C抑制剂1-(5-异喹啉磺酰基)-2-甲基哌嗪二盐酸盐(H-7)对大鼠肝切片中[3H]地塞米松核结合及糖皮质激素受体磷酸化的影响,以确定蛋白激酶C在糖皮质激素作用表达中的作用。H-7可降低大鼠肝切片中[3H]地塞米松的核结合。在不存在或存在糖皮质激素的情况下,它均不影响糖皮质激素受体的磷酸化程度。这些发现表明,蛋白激酶C可能参与糖皮质激素受体的核结合,但不直接影响受体磷酸化。

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