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K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases.
K-252a was a non-selective inhibitor for these three protein kinases with Ki values 18-25 nM, whereas K-252b showed a comparable potency for protein kinase C (Ki, 20nM), whereas inhibitory potencies for cyclic nucleotide-dependentprotein kinases were reduced.
Molecular characterization of a novel metabotropic glutamate receptor mGluR5 coupled to inositol phosphate/Ca2+ signal transduction.
It is demonstrated that there is an additional mGLUR subtype which closely resembles mGluR1 in its signal transduction and pharmacological properties and is expressed in specialized neuronal cells in the central nervous system.
Molecular characterization of a novel retinal metabotropic glutamate receptor mGluR6 with a high agonist selectivity for L-2-amino-4-phosphonobutyrate.
Blot and in situ hybridization analyses indicated that mGluR6 mRNA is restrictedly expressed in the inner nuclear layer of the retina where ON-bipolar cells are distributed, and the physiological role of this receptor subtype in the visual system is discussed.
Immunohistochemical localization of substance P receptor in the central nervous system of the adult rat
The findings confirmed the presence of the “ismatch” problem between SP and SPR localizations and indicated that the sites of SPR‐LI revealed in the present study represent most, if not all, sites of SP‐binding activity.
Signal transduction, pharmacological properties, and expression patterns of two rat metabotropic glutamate receptors, mGluR3 and mGluR4
The metabotropic glutamate receptors are coupled to intracellular signal transduction via G-proteins and consist of a family of at least five different subtypes, termed mGluR1-mGluR5. We studied the
Inhibition of histamine secretion by wortmannin through the blockade of phosphatidylinositol 3-kinase in RBL-2H3 cells.
The results suggest that PI3-kinase is involved in the signal transduction pathway responsible for histamine secretion following stimulation of Fc epsilon RI and that wortmannin blocks these responses through direct interaction with the catalytic subunit of this enzyme.
Differential expression of five N‐methyl‐D‐aspartate receptor subunit mRNAs in the cerebellum of developing and adult rats
The expression patterns of mRNAs for the NMDA receptor subunits in the developing and adult rats by in situ hybridization were analyzed and developmental changes of the expression patterns were most salient in the cerebellum.
A wortmannin-sensitive phosphatidylinositol 4-kinase that regulates hormone-sensitive pools of inositolphospholipids.
The results indicate that a specific WT-sensitive PtdIns 4-kinase is critical for the maintenance of the agonist-sensitive polyphosphoinositide pool in several cell types.
Impairment of Hippocampal Mossy Fiber LTD in Mice Lacking mGluR2
The mutant mice performed normally in water maze learning tasks and the presynaptic mGluR2 is essential for inducing LTD at the mossy fiber—CA3 synapses, but this hippocampal LTD does not seem to be required for spatial learning.
Wortmannin, a microbial product inhibitor of myosin light chain kinase.
Wortmannin inhibited both the phosphorylation of myosin light chain and the contraction in rat thoracic aorta stimulated with KCl, which indicates the effectiveness of the compound in the cellular level as an MLCK inhibitor.