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Chemical Compound Review

Lopac-D-5919     3-[2-[4-[(4-fluorophenyl)- phenyl...

Synonyms: Tocris-2194, CHEMBL259388, SureCN316891, AG-K-43092, D5919_SIGMA, ...
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Disease relevance of diacylglycerol kinase inhibitor i


Psychiatry related information on diacylglycerol kinase inhibitor i

  • R 59022, a compound which causes the accumulation of diacylglycerol by inhibition of the enzyme diacylglycerol kinase, was tested for its effect on stimulated motor activity of the longitudinal muscle from the guinea-pig ileum [4].

High impact information on diacylglycerol kinase inhibitor i

  • Treatment of cells with two DAG kinase inhibitors, R59022 and R59949, blocked the IGF-I-dependent rise in nuclear DAG kinase activity and maintained elevated intranuclear levels of DAG [5].
  • Membrane-permeant diacylglycerol analogues, which activated but did not down-regulate PKC, were devoid of growth-stimulating effects on melanocytes, even in the presence of the specific diacylglycerol kinase inhibitor, R59022 [6].
  • In the present studies, we investigated in these cells protein phosphorylation stimulated by various protein kinase C activators, including 1-oleoyl-2-acetylglycerol in the presence of the diacylglycerol kinase inhibitor R59022, TPA, mezerein, and bryostatin [7].
  • AtDGK7 activity was affected by pH, detergents, and the DGK inhibitor R59022 [8].
  • Furthermore, re-translocation of PKCgamma was obviously hastened by co-expression with DGKgamma and was blocked by an inhibitor of DGK (R59022) [9].

Biological context of diacylglycerol kinase inhibitor i

  • However, R59022, a DG kinase inhibitor, did not influence the accumulation of DG or PA, suggesting that platelet-derived growth factor stimulates mainly phospholipase D-catalyzed hydrolysis of phospholipids rather than phospholipase C-catalyzed hydrolysis in the second phase [10].
  • It is concluded that in studies on the signal-transducing system coupled to inositol lipid metabolism R 59 022 might occupy a role comparable to cyclic AMP phosphodiesterase inhibitors, since it potentiates the effect of the putative second messenger diacylglycerol by preventing its rapid metabolism [11].
  • Arabidopsis AtDGK7, the smallest member of plant diacylglycerol kinases (DGKs), displays unique biochemical features and saturates at low substrate concentration: the DGK inhibitor R59022 differentially affects AtDGK2 and AtDGK7 activity in vitro and alters plant growth and development [8].
  • In spermatozoa stimulated with Ca2+/A23187 and the DAG kinase inhibitor R59022, a similar increase in DAG levels together with stimulation of acrosomal exocytosis were observed [12].
  • The putative DGK inhibitor R59022 inhibited the 80-kDa DGK (IC50, 10 microM), but had little effect on the 150-kDa form [13].

Anatomical context of diacylglycerol kinase inhibitor i


Associations of diacylglycerol kinase inhibitor i with other chemical compounds

  • The diacylglycerol kinase inhibitors, dioctanoylethylene glycol and R59022 potentiated PLD stimulation by exogenous diacylglycerol but not by V(4+)-OOH [19].
  • Phosphorylation of myosin light chains, formation of inositol phosphates and the mobilization of Ca2+ by thrombin are not affected by R59022 (10 microM) [20].
  • Early DAG rises temporally overlapped respiratory burst initiation but PMN responses to hyphae were unchanged by a DAG kinase inhibitor, R59022, which blocks phosphorylation of DAG to PA and enhances DAG accumulation [21].
  • The temporal relationship of the evolution of PA and DAG is further strengthened by experiments with ethanol and propranolol as inhibitors of the DAG/PA phosphohydrolase reaction and R59022 as an inhibitor of the DAG kinase reaction [22].
  • The PMA effects could be mimicked by oleoylacetylglycerol, the diacylglycerol kinase inhibitor R59022 and exogenous phospholipase C. Treatment with PMA did not affect GABA transport in neuronal cells [23].

Gene context of diacylglycerol kinase inhibitor i

  • In contrast, bFGF stimulated the phosphorylation of the Mr 80,000 (80K) cellular protein which is a major substrate of protein kinase C. This effect was potentiated by the diacylglycerol kinase inhibitor R59022 [24].
  • The DGK inhibitor, R59022, inhibited DGK-II and to a lesser extent DGK-III, but little affected DGK-I activity [25].
  • A diacylglycerol kinase inhibitor, R 59 022, potentiates superoxide anion production and 46-kDa protein phosphorylation in guinea pig polymorphonuclear leukocytes [14].
  • R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet [11].
  • R59022 (10 microM), which inhibits DG kinase and causes accumulation of endogenous DGs, inhibited the KCl-induced rise in [Ca2+]i to 2 +/- 0.2% of the control value; this inhibition was not affected by staurosporine [26].

Analytical, diagnostic and therapeutic context of diacylglycerol kinase inhibitor i

  • To demonstrate that these effects were mediated by PKC activation, PKC isoforms were measured by Western blotting following R59022 exposure (50 mumol/l, 30 min) [27].


  1. Intracellular calcium mobilization and phospholipid degradation in sphingosylphosphorylcholine-stimulated human airway epithelial cells. Orlati, S., Porcelli, A.M., Hrelia, S., Lorenzini, A., Rugolo, M. Biochem. J. (1998) [Pubmed]
  2. Effects of bradykinin, GTP gamma S, R59022 and N-ethylmaleimide on inositol phosphate production in NG108-15 cells. Chiang, C.F., Hauser, G. Biochem. Biophys. Res. Commun. (1989) [Pubmed]
  3. Shape changes and chemokinesis of Walker carcinosarcoma cells: effects of protein kinase inhibitors (HA-1004, polymyxin B, sangivamycin and tamoxifen) and an inhibitor of diacylglycerol kinase (R 59022). Zimmermann, A., Keller, H. Anticancer Res. (1993) [Pubmed]
  4. The diacylglycerol kinase inhibitor, R 59022, suppresses contractility of intestinal smooth muscle. Lippe, I.T., Holzer, P. Eur. J. Pharmacol. (1989) [Pubmed]
  5. Enhanced nuclear diacylglycerol kinase activity in response to a mitogenic stimulation of quiescent Swiss 3T3 cells with insulin-like growth factor I. Martelli, A.M., Tabellini, G., Bortul, R., Manzoli, L., Bareggi, R., Baldini, G., Grill, V., Zweyer, M., Narducci, P., Cocco, L. Cancer Res. (2000) [Pubmed]
  6. Protein kinase C down-regulation, and not transient activation, correlates with melanocyte growth. Brooks, G., Wilson, R.E., Dooley, T.P., Goss, M.W., Hart, I.R. Cancer Res. (1991) [Pubmed]
  7. Differential effects of various protein kinase C activators on protein phosphorylation in human acute myeloblastic leukemia cell line KG-1 and its phorbol ester-resistant subline KG-1a. Kiss, Z., Deli, E., Shoji, M., Koeffler, H.P., Pettit, G.R., Vogler, W.R., Kuo, J.F. Cancer Res. (1987) [Pubmed]
  8. Arabidopsis AtDGK7, the smallest member of plant diacylglycerol kinases (DGKs), displays unique biochemical features and saturates at low substrate concentration: the DGK inhibitor R59022 differentially affects AtDGK2 and AtDGK7 activity in vitro and alters plant growth and development. Gómez-Merino, F.C., Arana-Ceballos, F.A., Trejo-Téllez, L.I., Skirycz, A., Brearley, C.A., Dörmann, P., Mueller-Roeber, B. J. Biol. Chem. (2005) [Pubmed]
  9. Subtype-specific translocation of diacylglycerol kinase alpha and gamma and its correlation with protein kinase C. Shirai, Y., Segawa, S., Kuriyama, M., Goto, K., Sakai, N., Saito, N. J. Biol. Chem. (2000) [Pubmed]
  10. Phosphatidic acid that accumulates in platelet-derived growth factor-stimulated Balb/c 3T3 cells is a potential mitogenic signal. Fukami, K., Takenawa, T. J. Biol. Chem. (1992) [Pubmed]
  11. R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet. de Chaffoy de Courcelles, D.C., Roevens, P., Van Belle, H. J. Biol. Chem. (1985) [Pubmed]
  12. The role of diacylglycerol in the exocytosis of the sperm acrosome. Studies using diacylglycerol lipase and diacylglycerol kinase inhibitors and exogenous diacylglycerols. Roldan, E.R., Harrison, R.A. Biochem. J. (1992) [Pubmed]
  13. Different effects of sphingosine, R59022 and anionic amphiphiles on two diacylglycerol kinase isozymes purified from porcine thymus cytosol. Sakane, F., Yamada, K., Kanoh, H. FEBS Lett. (1989) [Pubmed]
  14. A diacylglycerol kinase inhibitor, R 59 022, potentiates superoxide anion production and 46-kDa protein phosphorylation in guinea pig polymorphonuclear leukocytes. Ohtsuka, T., Hiura, M., Yoshida, K., Okamura, N., Ishibashi, S. J. Biol. Chem. (1990) [Pubmed]
  15. Involvement of protein kinase C and protein tyrosine kinase in lipopolysaccharide-induced TNF-alpha and IL-1 beta production by human monocytes. Shapira, L., Takashiba, S., Champagne, C., Amar, S., Van Dyke, T.E. J. Immunol. (1994) [Pubmed]
  16. Novel diacylglycerol kinase inhibitor selectively suppressed an U46619-induced enhancement of mouse portal vein contraction under high glucose conditions. Nobe, K., Miyatake, M., Nobe, H., Sakai, Y., Takashima, J., Momose, K. Br. J. Pharmacol. (2004) [Pubmed]
  17. Increased protein synthesis response to insulin in fibroblasts treated with the diacylglycerol kinase inhibitor R59022. Hesketh, J.E., McKenzie, N., Campbell, G.P. FEBS Lett. (1988) [Pubmed]
  18. Effects of prolonged EGF treatment on phospholipid turnover and DAG formation in murine keratinocytes. Punnonen, K., Isoherranen, K., Laihia, J., Leino, L. Cell. Signal. (1996) [Pubmed]
  19. Peroxides of vanadate induce activation of phospholipase D in HL-60 cells. Role of tyrosine phosphorylation. Bourgoin, S., Grinstein, S. J. Biol. Chem. (1992) [Pubmed]
  20. A diacylglycerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human platelets. Nunn, D.L., Watson, S.P. Biochem. J. (1987) [Pubmed]
  21. Relationship of phospholipase C- and phospholipase D-mediated phospholipid remodeling pathways to respiratory burst activation in human neutrophils stimulated by Candida albicans hyphae. Meshulam, T., Billah, M.M., Eckel, S., Griendling, K.K., Diamond, R.D. J. Leukoc. Biol. (1995) [Pubmed]
  22. Erythropoietin stimulates G-protein-coupled phospholipase D in haematopoietic target cells. Clejan, S., Mallia, C., Vinson, D., Dotson, R., Beckman, B.S. Biochem. J. (1996) [Pubmed]
  23. Inhibition of high-affinity gamma-aminobutyric acid uptake in primary astrocyte cultures by phorbol esters and phospholipase C. Gomeza, J., Casado, M., Gimenez, C., Aragon, C. Biochem. J. (1991) [Pubmed]
  24. Fibroblast growth factor stimulates protein kinase C in quiescent 3T3 cells without Ca2+ mobilization or inositol phosphate accumulation. Nånberg, E., Morris, C., Higgins, T., Vara, F., Rozengurt, E. J. Cell. Physiol. (1990) [Pubmed]
  25. Purification and characterization of cytosolic diacylglycerol kinases of human platelets. Yada, Y., Ozeki, T., Kanoh, H., Nozawa, Y. J. Biol. Chem. (1990) [Pubmed]
  26. Diacylglycerol inhibits potassium-induced calcium influx and insulin release by a protein kinase-C-independent mechanism in HIT T-15 islet cells. Thomas, T.P., Pek, S.B. Endocrinology (1992) [Pubmed]
  27. Effects of the diacylglycerol kinase inhibitor, R59022, on TSH-stimulated iodide organification in porcine thyroid cells. Matowe, W.C., Ginsberg, J. Pharmacology (1996) [Pubmed]
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