Tyrphostins inhibit the epidermal growth factor receptor-mediated breakdown of phosphoinositides

Israel Posner; Aviv Gazit; Chaim Gilon; Alexander Levitzki

doi:10.1016/0014-5793(89)81554-6

Tyrphostins inhibit the epidermal growth factor receptor-mediated breakdown of phosphoinositides

Israel Posner
, Aviv Gazit
, Chaim Gilon
, Alexander Levitzki^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

33 Scopus citations

Abstract

In response to epidermal growth factor (EGF) and the Ca²⁺ ionophore A23187, the total phosphatidylinositides (IPT) increased in A431 human epidermoid carcinoma cells 1.8- and 2.0-fold and in the EGF-dependent A431/Clone 15-2 cells 3.0- and 8.0-fold, respectively, over basal levels. Both responses were inhibited by the antiproliferative agents tyrphostins, but the EGF-induced increase in IP_T was inhibited to a much greater extent than that induced by the ionophore. Tyrphostins which are potent EGF-receptor kinase inhibitors were also potent in blocking the EGF-induced production of phosphoinositides. The less potent tyrphostins were found to inhibit the EGF-dependent IP_T formation more weakly. These results support the notion that phospholipase C is activated through its phosphorylation by the EGF receptor. Tyrphostins; Epidermal growth factor; Phospholipase C phosphorylation; Ca²⁺ ionophore; (A431 cell, A431/Clone 15-2 cell).

Original language	English
Pages (from-to)	287-291
Number of pages	5
Journal	FEBS Letters
Volume	257
Issue number	2
DOIs	https://doi.org/10.1016/0014-5793(89)81554-6
State	Published - 6 Nov 1989

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title = "Tyrphostins inhibit the epidermal growth factor receptor-mediated breakdown of phosphoinositides",

abstract = "In response to epidermal growth factor (EGF) and the Ca2+ ionophore A23187, the total phosphatidylinositides (IPT) increased in A431 human epidermoid carcinoma cells 1.8- and 2.0-fold and in the EGF-dependent A431/Clone 15-2 cells 3.0- and 8.0-fold, respectively, over basal levels. Both responses were inhibited by the antiproliferative agents tyrphostins, but the EGF-induced increase in IPT was inhibited to a much greater extent than that induced by the ionophore. Tyrphostins which are potent EGF-receptor kinase inhibitors were also potent in blocking the EGF-induced production of phosphoinositides. The less potent tyrphostins were found to inhibit the EGF-dependent IPT formation more weakly. These results support the notion that phospholipase C is activated through its phosphorylation by the EGF receptor. Tyrphostins; Epidermal growth factor; Phospholipase C phosphorylation; Ca2+ ionophore; (A431 cell, A431/Clone 15-2 cell).",

author = "Israel Posner and Aviv Gazit and Chaim Gilon and Alexander Levitzki",

year = "1989",

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AU - Posner, Israel

AU - Gazit, Aviv

AU - Gilon, Chaim

AU - Levitzki, Alexander

PY - 1989/11/6

Y1 - 1989/11/6

N2 - In response to epidermal growth factor (EGF) and the Ca2+ ionophore A23187, the total phosphatidylinositides (IPT) increased in A431 human epidermoid carcinoma cells 1.8- and 2.0-fold and in the EGF-dependent A431/Clone 15-2 cells 3.0- and 8.0-fold, respectively, over basal levels. Both responses were inhibited by the antiproliferative agents tyrphostins, but the EGF-induced increase in IPT was inhibited to a much greater extent than that induced by the ionophore. Tyrphostins which are potent EGF-receptor kinase inhibitors were also potent in blocking the EGF-induced production of phosphoinositides. The less potent tyrphostins were found to inhibit the EGF-dependent IPT formation more weakly. These results support the notion that phospholipase C is activated through its phosphorylation by the EGF receptor. Tyrphostins; Epidermal growth factor; Phospholipase C phosphorylation; Ca2+ ionophore; (A431 cell, A431/Clone 15-2 cell).

AB - In response to epidermal growth factor (EGF) and the Ca2+ ionophore A23187, the total phosphatidylinositides (IPT) increased in A431 human epidermoid carcinoma cells 1.8- and 2.0-fold and in the EGF-dependent A431/Clone 15-2 cells 3.0- and 8.0-fold, respectively, over basal levels. Both responses were inhibited by the antiproliferative agents tyrphostins, but the EGF-induced increase in IPT was inhibited to a much greater extent than that induced by the ionophore. Tyrphostins which are potent EGF-receptor kinase inhibitors were also potent in blocking the EGF-induced production of phosphoinositides. The less potent tyrphostins were found to inhibit the EGF-dependent IPT formation more weakly. These results support the notion that phospholipase C is activated through its phosphorylation by the EGF receptor. Tyrphostins; Epidermal growth factor; Phospholipase C phosphorylation; Ca2+ ionophore; (A431 cell, A431/Clone 15-2 cell).

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Tyrphostins inhibit the epidermal growth factor receptor-mediated breakdown of phosphoinositides

Abstract

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