A23187对胰岛素受体结合的抑制作用：与佛波酯的协同作用。

Inhibition of insulin receptor binding by A23187: synergy with phorbol esters.

作者信息

Rouis M, Thomopoulos P, Cherier C, Testa U

出版信息

Biochem Biophys Res Commun. 1985 Jul 16;130(1):9-15. doi: 10.1016/0006-291x(85)90374-2.

Abstract

The ionophore A23187 inhibits the binding of insulin on U-937 monocyte-like cells which had been induced to differentiate by 1 alpha, 25-(OH)2 cholecalciferol, while it remains inactive on the undifferentiated cells. A 50% reduction of the specific binding of 125I-insulin is observed within 20 to 30 min at 37 degrees C. The effect is obtained at 10(-7)M to 10(-6)M A23187. It is reversible in 60 min at 37 degrees C. A suboptimal concentration of the ionophore potentiates the inhibitory action of phorbol esters on insulin binding.

摘要

离子载体A23187可抑制胰岛素与经1α,25 - (OH)₂胆钙化醇诱导分化的U - 937单核细胞样细胞的结合，而对未分化细胞则无活性。在37℃下，20至30分钟内可观察到¹²⁵I - 胰岛素特异性结合减少50%。在10⁻⁷M至10⁻⁶M的A23187浓度下可产生该效应。在37℃下60分钟内该效应可逆。离子载体的次优浓度可增强佛波酯对胰岛素结合的抑制作用。