INHIBITION OF PROTEIN-KINASE-C BY CALPHOSTIN-C IS LIGHT-DEPENDENT
INHIBITION OF PROTEIN-KINASE-C BY CALPHOSTIN-C IS LIGHT-DEPENDENT
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DOI：
10.1016/0006-291x(91)90922-t
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发表时间：
1991-04-15
影响因子：
3.1
通讯作者：
NAKANO, H
中科院分区：
文献类型：
--
作者：
BRUNS, RF;MILLER, FD;NAKANO, H
Calphostin C是枝孢霉Cladosporium cladosporioides的次级代谢产物，通过竞争甘油二酯和佛波醇酯的结合位点来抑制蛋白激酶C。Calphostin C是一种多环碳氢化合物，在可见光和紫外线范围内具有强吸收性。在表征该化合物的活性时，我们意外地发现[3 H]佛波醇二丁酸酯结合的抑制依赖于暴露于光。普通的荧光灯就足够了。在无细胞系统和完整细胞中蛋白激酶C活性的抑制也需要光。在比抑制蛋白激酶C的浓度高约5倍的浓度下观察到光依赖性细胞毒性。
Calphostin C, a secondary metabolite of the fungusCladosporium cladosporioides, inhibits protein kinase C by competing at the binding site for diacylglycerol and phorbol esters. Calphostin C is a polycyclic hydrocarbon with strong absorbance in the visible and ultraviolet ranges. In characterizing the activity of this compound, we unexpectedly found that the inhibition of [3H]phorbol dibutyrate binding was dependent on exposure to light. Ordinary fluorescent light was sufficient for full activation. The inhibition of protein kinase C activity in cell-free systems and intact cells also required light. Light-dependent cytotoxicity was seen at concentrations about 5-fold higher than those inhibiting protein kinase C.