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Protein kinase C (PKC) inhibitor Calphostin C activates PKC in a light-dependent manner at high concentrations via the production of singlet oxygen.
Eur J Pharmacol
December 2024
Department of Molecular and Pharmacological Neuroscience, Graduate School of Biomedical & Health Sciences, Hiroshima University, Japan. Electronic address:
Article Synopsis
- Calphostin C (Cal-C) is a known protein kinase C (PKC) inhibitor that can inhibit PKC activation at low concentrations but activate it at high concentrations through a light-dependent mechanism.
- At low doses (<200 nM), Cal-C successfully stops PKC translocation and activation induced by certain compounds, while at higher doses (>2 μM), it raises intracellular calcium levels by mobilizing the endoplasmic reticulum (ER) without involving specific receptors.
- The study also found that high concentrations of Cal-C cause structural changes in the ER and generate singlet oxygen, which contributes to PKC activation and indicates its potential use in photodynamic therapy.
PKCβII activation requires nuclear trafficking for phosphorylation and Mdm2-mediated ubiquitination.
Life Sci Alliance
April 2023
Department of Pharmacology, College of Pharmacy, Chonnam National University, Gwang-Ju, Republic of Korea
PKCβII, a conventional PKC family member, plays critical roles in the regulation of a variety of cellular functions. Here, we employed loss-of-function approaches and mutants of PKCβII with altered phosphorylation and protein interaction behaviors to identify the cellular mechanisms underlying the activation of PKCβII. Our results show that 3-phosphoinositide-dependent protein kinase-1 (PDK1)-mediated constitutive phosphorylation of PKCβII at the activation loop (T500) is required for phorbol ester-induced nuclear entry and subsequent Mdm2-mediated ubiquitination of PKCβII, whereas ubiquitination of PKCβII is required for the PDK1-mediated inducible phosphorylation of PKCβII at T500 in the nucleus.
View Article and Find Full Text PDFThe Y14-p53 regulatory circuit in megakaryocyte differentiation and thrombocytopenia.
iScience
November 2021
Institute of Biomedical Sciences, Academia Sinica, 128 Academia Road, Section 2, Nangang, Taipei 11529, Taiwan.
Thrombocytopenia-absent radius (TAR) syndrome is caused by RBM8A insufficiency. We generated megakaryocyte-specific knockout (KO) mice that exhibited marked thrombocytopenia, internal hemorrhage, and splenomegaly, providing evidence that genetic deficiency of causes a disorder of platelet production. KO mice accumulated low-ploidy immature megakaryocytes in the bone marrow and exhibited defective platelet activation and aggregation.
View Article and Find Full Text PDFMolecular dynamics simulation studies on binding of activator and inhibitor to Munc13-1 C1 in the presence of membrane.
J Biomol Struct Dyn
December 2022
Department of Pharmacological & Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX, USA.
Munc13-1 is a presynaptic active zone protein that plays a critical role in priming the synaptic vesicle and releasing neurotransmitters in the brain. Munc13-1 acts as a scaffold and is activated when diacylglycerol (DAG)/phorbol ester binds to its C1 domain in the plasma membrane. Our previous studies showed that bryostatin 1 activated the Munc13-1, but resveratrol inhibited the phorbol ester-induced Munc13-1 activity.
View Article and Find Full Text PDFActivation of activator protein-1-fibroblast growth factor 21 signaling attenuates Cisplatin hepatotoxicity.
Biochem Pharmacol
December 2021
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY 11439, United States. Electronic address:
Fibroblast growth factor (Fgf/FGF) 21, which plays important roles in sugar, lipid and energy metabolism, has been accepted as a mito-stress marker gene. We recently reported that FGF21 expression can be up-regulated via activation of aryl hydrocarbon receptor (AhR) or glucocorticoid receptor (GR) and that FGF21 plays important cytoprotective roles. Cisplatin (cis-diamminedichloroplatinum, CDDP) is a widely used chemotherapeutic drug.
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