| Yuanhuacin A Is a Selective Antagonist of Phorbol Ester Receptor in Protein Kinase C |
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| 引用本文： | 张德昌,曹春霞,张春姜,周炳南. Yuanhuacin A Is a Selective Antagonist of Phorbol Ester Receptor in Protein Kinase C[J]. 中国科学B辑(英文版), 1993, 0(7) |
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| 作者姓名： | 张德昌 曹春霞 张春姜 周炳南 |
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| 作者单位： | Institute of Basic Medical Sciences，Chinese Academy of Medical Sciences，Beijing 100730，PRC，Institute of Basic Medical Sciences，Chinese Academy of Medical Sciences，Beijing 100730，PRC，Institute of Basic Medical Sciences，Chinese Academy of Medical Sciences，Beijing 100730，PRC，Shanghai Institute of Materia Medica，Academia Sinica，Shanghai 200031，PRC |
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| 摘 要： | Protein kinase C with a molecular weight of 82 kD has been purified to electrophoresis homogenous from rat brain through a series of chromatography columns including DE-52, Sepharose G-200 and phenyl-Sepharose. The enzyme possessed autophosphorylation activity. Yuanhuacin A inhibited the ~3H-phorbol-12, 13-dibutyrate (~3H-PdBu) binding of PKC with an IC_(50) value of 1.48±0.28×10~(-8) mol/L when the concentration of ~3H-PdBu was 1.5×10~(-9) mol/L (K_i=1.2×10~(-8) mol/L). Yuanhuacin A inhibited the PdBu-stimulated PKC activity in the catalysis of the phosphorylation of Histone Ⅲ-S with an IC_(50) of 2.82±0.37×10~(-9) mol/L (PdBu=10~(-6) mol/L), while it had no effect on the basal and Ca~(2+)-stimulated PKC activity in the same assay system. This result suggests that Yuanhuacin A is a selective antagonist of the phorbol ester receptor in protein kinase C.
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Yuanhuacin A Is a Selective Antagonist of Phorbol Ester Receptor in Protein Kinase C |
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| ZHANG De-Chang CAO Chun-XiaZHANG Chun-Jiang. Yuanhuacin A Is a Selective Antagonist of Phorbol Ester Receptor in Protein Kinase C[J]. Science in China(Chemistry), 1993, 0(7) |
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| Authors: | ZHANG De-Chang CAO Chun-XiaZHANG Chun-Jiang |
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| Abstract: | |
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| Keywords: | protein kinase C phorbol esters Yuanhuaein A ~3H-phorbol-12 13-dibutyrate. |
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