O'Flaherty J T, Jacobson D
Department of Medicine, Wake Forest University Medical Center, Winston-Salem, NC 27103.
Biochem Biophys Res Commun. 1989 Sep 29;163(3):1456-60. doi: 10.1016/0006-291x(89)91142-x.
Three protein kinase C blockers (staurosporin, Cl, and sphinganine) acted temperature- and time-dependently on human neutrophils to lower the affinity and number of high affinity plasmalemma receptors available to leukotriene B4. The drugs did not alter the ligand's binding to isolated plasma membranes or reduce intact cell binding of platelet-activating factor. Thus, protein kinase C may regulate the expression of certain receptors in resting cells and blockers of this enzyme, by interfering with receptor expression, have secondary effects that complicate their use as pharmacological probes.
三种蛋白激酶C阻断剂(星形孢菌素、氯和鞘氨醇)对人中性粒细胞的作用具有温度和时间依赖性,可降低白三烯B4可利用的高亲和力质膜受体的亲和力和数量。这些药物不会改变配体与分离的质膜的结合,也不会降低血小板活化因子在完整细胞上的结合。因此,蛋白激酶C可能调节静息细胞中某些受体的表达,而这种酶的阻断剂通过干扰受体表达,会产生一些副作用,使其作为药理学探针的应用变得复杂。