The linoleic acid derivative DCP-LA selectively activates PKC-epsilon, possibly binding to the phosphatidylserine binding site.

Journal of Lipid Research
Takeshi KannoTomoyuki Nishizaki

Abstract

This study examined the effect of 8-[2-(2-pentyl-cyclopropylmethyl)-cyclopropyl]-octanoic acid (DCP-LA), a newly synthesized linoleic acid derivative with cyclopropane rings instead of cis-double bonds, on protein kinase C (PKC) activity. In the in situ PKC assay with reverse-phase high-performance liquid chromatography, DCP-LA significantly activated PKC in PC-12 cells in a concentration-dependent (10 nM-100 microM) manner, with the maximal effect at 100 nM, and the DCP-LA effect was blocked by GF109203X, a PKC inhibitor, or a selective inhibitor peptide of the novel PKC isozyme PKC-epsilon. Furthermore, DCP-LA activated PKC in HEK-293 cells that was inhibited by the small, interfering RNA against PKC-epsilon. In the cell-free PKC assay, of the nine isozymes examined here, DCP-LA most strongly activated PKC-epsilon, with >7-fold potency over other PKC isozymes, in the absence of dioleoyl-phosphatidylserine and 1,2-dioleoyl-sn-glycerol; instead, the DCP-LA action was inhibited by dioleoyl-phosphatidylserine. DCP-LA also activated PKC-gamma, a conventional PKC, but to a much lesser extent compared with that for PKC-epsilon, by a mechanism distinct from PKC-epsilon activation. Thus, DCP-LA serves as a selective activator of PKC-e...Continue Reading

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Citations

Jun 12, 2013·Lipids·Tomasz SledzinskiJulian Swierczynski
Dec 3, 2013·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Thomas J NelsonMiao-Kun Sun
Oct 24, 2009·The Journal of Biological Chemistry·Thomas J NelsonDaniel L Alkon
Mar 15, 2012·Cellular Physiology and Biochemistry : International Journal of Experimental Cellular Physiology, Biochemistry, and Pharmacology·Takeshi KannoTomoyuki Nishizaki
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Aug 27, 2013·PloS One·Farshad TamariYiannis A Ioannou
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Feb 24, 2009·Trends in Biochemical Sciences·T J Nelson, D L Alkon
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Nov 1, 2007·Journal of Neurochemistry·Kristof Van KolenFrank M Dautzenberg
Nov 10, 2009·Archiv der Pharmazie·Miao-Kun Sun, Daniel L Alkon
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