Imidazole antimycotics inhibitors of cytochrome P450 increase phosphatidylserine synthesis similarly to K+‐channel blockers in Jurkat T cells

FEBS Letters

Breittmayer, Jean Philippe¹  Aussel, Claude¹ 

[1] INSERM U343, Interactions cellulaires en Immunologie, Faculté de Médecine, 06107 Nice Cédex, France

关键词: K+ channel;    Ca2+ channel;    Cytochrome P450;    Antimycotics;    Phosphatidylserine;    Membrane potential;   

DOI  :  10.1016/0014-5793(93)80057-2

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The imidazole antimycotics, miconazole, econazole and triclomazole as well as α-naphtoflavone, known as powerful inhibitors of cytochrome P₄₅₀ and previously recognized as K⁺ channel blockers are shown to be potent activators of the base exchange enzyme system responsible for the biosynthesis of phosphatidylserine in Jurkat T cells. The inhibition of CD3-induced Ca²⁺ influx by antimycotics but not by K⁺ channel blockers, demonstrated that the rise in phosphatidylserine synthesis caused by the two classes of drugs, was independent of Ca²⁺ influx in the cells. In addition, we show that the action of these drugs on phosphatidylserine synthesis was not mimicked by modifications of membrane potential. The regulation of both K⁺ channels and the base exchange enzyme system thus occurs through a similar (or common) pathway that is independent of Ca²⁺-influx and membrane potential.

【 授权许可】

Unknown