Inhibitors of diacylglycerol kinase from Drechslera sacchari.

THE JOURNAL OF ANTIBIOTICS INHIBITORS OF DIACYLGLYCEROL KINASEFROMDrechslera sacchari

Cells respond to a variety of signals by activation of a phospholipase C which catalyzes the phosphodiesteric cleavage of phosphatidylinositol 4,5bisphosphate to generate intracellular second messengers, inositol 1,4,5-trisphosphate and 1,2diacylglycerol. Previously, we described the isolation of an inhibitor for inositol-specific phospholipase C from Actinomadura sp. This inhibitor therefore m...

Cochlioquinone A, an inhibitor of diacylglycerol kinase.

The effects of cochlioquinone A, isolated from Drechslera sacchari, were studied in vitro and in vivo. This compound specifically inhibited diacylglycerol kinase activity with Ki = 3.1 microM. The kinetics revealed that cochlioquinone A inhibited diacylglycerol kinase in competition with ATP, and non-competitively with diacylglycerol. The compound inhibited neither protein kinase C, epidermal g...

Editorial: Diacylglycerol Kinase Signalling

The role of diacylglycerol in the exocytosis of the sperm acrosome. Studies using diacylglycerol lipase and diacylglycerol kinase inhibitors and exogenous diacylglycerols.

When ram spermatozoa were treated with Ca2+ and the ionophore A23187 to induce acrosomal exocytosis, a rise in diacylglycerol (DAG) mass was observed, concomitant with a rapid breakdown of [32P]P1-labelled phosphatidylinositol 4,5-bisphosphate and phosphatidylinositol 4-phosphate and a rise in [32P]Pi-labelled phosphatidate. Inclusion of the DAG lipase inhibitor RHC 80267 resulted in further bu...

Diacylglycerol kinase ζ controls diacylglycerol metabolism at the immunological synapse

Diacylglycerol (DAG) generation at the T cell immunological synapse (IS) determines the correct activation of antigen-specific immune responses. DAG kinases (DGKs) α and ζ act as negative regulators of DAG-mediated signals by catalyzing DAG conversion to phosphatidic acid (PA). Nonetheless, the specific input of each enzyme and their spatial regulation during IS formation remain uncharacterized...