title: Effects of newly synthesized DCP-LA-phospholipids on protein kinase C and protein phosphatases.
abstract: OBJECTIVE
  The linoleic acid derivative DCP-LA selectively activates PKCε and inhibits protein phosphatase 1 (PP1). In the present study, we have newly synthesized phosphatidyl-ethanolamine, -serine, -choline, and -inositol containing DCP-LA at the α and β position (diDCP-LA-PE, -PS, PC, and -PI, respectively), and examined the effects of these compounds on activities of PKC isozymes and protein phosphatases.
  
  
  METHODS
  Activities of PKC isozymes PKCα, -βΙ, -βΙΙ, -γ, -δ, -ε-, ι, and -ζ and protein phosphatases PP1, PP2A, and protein tyrosine phosphatase 1B (PTP1B) were assayed under the cell-free conditions.
  
  
  RESULTS
  All the compounds activated PKC, with the different potential, but only PKCγ inhibition was obtained with diDCP-LA-PC. Of compounds diDCP-LA-PE alone significantly activated PKCι and -ζ. diDCP-LA-PE and diDCP-LA-PI suppressed PP1 activity, but otherwise diDCP-LA-PI enhanced PP2A activity. diDCP-LA-PE, diDCP-LA-PS, and diDCP-LA-PI strongly reduced PTP1B activity, while diDCP-LA-PC enhanced the activity.
  
  
  CONCLUSIONS
  All the newly synthesized DCP-LA-phospholipids serve as a PKC activator and of them diDCP-LA-PE alone has the potential to activate the atypical PKC isozymes PKCι and -ζ. diDCP-LA-PE and diDCP-LA-PI serve as an inhibitor for PP1 and PTP1B, diDCP-LA-PS as a PTP1B inhibitor, diDCP-LA-PI as a PP2A enhancer, and diDCP-LA-PC as a PTP1B enhancer.
authors.affiliation: Division of Bioinformation, Department of Physiology, Hyogo College of Medicine, 1-1 Mukogawa-cho, Nishinomiya 663-8501, Japan.
authors.forename: Takeshi
authors.initials: T
authors.lastname: Kanno
authors.forename: Ayako
authors.initials: A
authors.lastname: Tsuchiya
authors.forename: Tadashi
authors.initials: T
authors.lastname: Shimizu
authors.forename: Syuhei
authors.initials: S
authors.lastname: Nakao
authors.forename: Akito
authors.initials: A
authors.lastname: Tanaka
authors.forename: Tomoyuki
authors.initials: T
authors.lastname: Nishizaki
mesh_terms: D002210:Caprylates / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D007527:Isoenzymes / Q000737:chemistry / Q000378:metabolism; D010714:Phosphatidylethanolamines / Q000737:chemistry* / Q000378:metabolism; D010749:Phosphoprotein Phosphatases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011485:Protein Binding; D011493:Protein Kinase C / Q000737:chemistry* / Q000378:metabolism; D054645:Protein Phosphatase 1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D054648:Protein Phosphatase 2 / Q000037:antagonists & inhibitors / Q000378:metabolism; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors / Q000378:metabolism
chemical_list: C000607905:1,2-O-bis(8-(2-(2-pentylcyclopropylmethyl)cyclopropyl)octanoyl)-sn-glycero-3-phosphatidylethanolamine; C506022:8-(2-(2-pentyl-cyclopropylmethyl)cyclopropyl)octanoic acid; D002210:Caprylates; D004791:Enzyme Inhibitors; D007527:Isoenzymes; D010714:Phosphatidylethanolamines; D011493:Protein Kinase C; D010749:Phosphoprotein Phosphatases; D054645:Protein Phosphatase 1; D054648:Protein Phosphatase 2; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1