Twomey B, Muid R E, Nixon J S, Sedgwick A D, Wilkinson S E, Dale M M
Department of Pharmacology, University College London, UK.
Biochem Biophys Res Commun. 1990 Sep 28;171(3):1087-92. doi: 10.1016/0006-291x(90)90795-o.
New potent inhibitors of protein kinase C were found to inhibit protein kinase C isolated from rat brain and human neutrophils, with a large degree of selectivity over cAMP-dependent kinase and Ca2+/calmodulin-dependent kinase. These novel compounds were potent inhibitors of the fluoride, diC8- and formyl-methionyl-leucyl-phenylalanine-mediated respiratory bursts in intact neutrophils. The opsonized zymosan-stimulated burst was only marginally affected by the compounds. These results differ from those obtained in studies with H7 and CI, (which are less potent and less specific protein kinase C inhibitors) and are consistent with the hypothesis that protein kinase C has a role in the transduction mechanism for the neutrophil oxidative burst stimulated with fluoride, formyl-methionyl-leucyl-phenylalanine and diC8.
新型强效蛋白激酶C抑制剂可抑制从大鼠脑和人中性粒细胞中分离出的蛋白激酶C,对环磷酸腺苷依赖性激酶和钙离子/钙调蛋白依赖性激酶具有高度选择性。这些新型化合物是完整中性粒细胞中氟化物、二辛酯和甲酰甲硫氨酰亮氨酰苯丙氨酸介导的呼吸爆发的强效抑制剂。经调理的酵母聚糖刺激的爆发仅受到这些化合物的轻微影响。这些结果与使用H7和CI(它们是效力较弱且特异性较差的蛋白激酶C抑制剂)的研究结果不同,并且与蛋白激酶C在由氟化物、甲酰甲硫氨酰亮氨酰苯丙氨酸和二辛酯刺激的中性粒细胞氧化爆发的转导机制中起作用的假设一致。