INHIBITION OF PROTEIN-KINASE-C BY CALPHOSTIN-C IS LIGHT-DEPENDENT

被引:402
作者
BRUNS, RF [1 ]
MILLER, FD [1 ]
MERRIMAN, RL [1 ]
HOWBERT, JJ [1 ]
HEATH, WF [1 ]
KOBAYASHI, E [1 ]
TAKAHASHI, I [1 ]
TAMAOKI, T [1 ]
NAKANO, H [1 ]
机构
[1] KYOWA HAKKO KOGYO CO LTD, TOKYO RES LABS, MACHIDA, TOKYO, JAPAN
关键词
D O I
10.1016/0006-291X(91)90922-T
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Calphostin C, a secondary metabolite of the fungus Cladosporium 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. © 1991.
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页码:288 / 293
页数:6
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