Ionotropic glutamate receptors mediate the majority of excitatory synaptic transmission in the brain and are thought to be involved in learning and memory formation. The activity of -amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA)-type glutamate receptors can be regulated by direct phosphorylation of their subunits, which affects the electrophysiological properties of the receptor, and t...

Conformational changes acutely control protein kinase C (PKC). We have previously shown that the autoinhibitory pseudosubstrate must be removed from the active site in order for 1) PKC to be phosphorylated by its upstream kinase phosphoinositide-dependent kinase 1 (PDK-1), 2) the mature enzyme to bind and phosphorylate substrates, and 3) the mature enzyme to be dephosphorylated by phosphatases....

We here describe the structural requirements for Golgi localization and a sequential, localization-dependent activation process of protein kinase C (PKC) mu involving auto- and transphosphorylation. The structural basis for Golgi compartment localization was analyzed by confocal microscopy of HeLa cells expressing various PKC mu-green fluorescent protein fusion proteins costained with the Golgi...

Platelet-activating factor (PAF) is a proinflammatory lipid that has both platelet- and phagocyte-stimulating properties. Because several known activators of calcium-, phospholipid-dependent protein kinase (protein kinase c, PKC) also stimulate neutrophil responses and because neutrophil stimuli such as phorbol diesters and the chemotactic peptide f-Met-Leu-Phe are reported to increase protein ...

Phosphorylation of cardiac myofibrillar proteins by protein kinase C (PKC) in isolated adult rat cardiomyocytes has been compared with that mediated by the cAMP-dependent protein kinase (PKA). PKA activation by beta-adrenoreceptor (isoproterenol) stimulation results in stoichiometric phosphorylation of troponin I (TnI) and C-protein. PKC activation by either 12-O-tetradecanoylphorbol-13-acetate...

We previously reported an increased secretion of amyloid precursor-like protein 2 (APLP2) in the healing corneal epithelium. The present study sought to investigate signal transduction pathways involved in APLP2 shedding in vitro. APLP2 was constitutively shed and released into culture medium in SV40-immortalized human corneal epithelial cells as assessed by Western blotting, flow cytometry, an...

Drugs that target protein kinase C (PKC) are now being evaluated in patients with non-small cell lung cancer (NSCLC), but the role of PKC in NSCLC cells remains unclear. We report here that NSCLC cell lines show enhanced phosphorylation and altered expression of specific PKC isoforms compared with normal lung epithelial cells. PKC inhibition variably increased apoptosis, with rottlerin, a PKCde...