Numerous efficacy studies in rodents revealed that 1,4-phenylenebis(methylene)-selenocyanat (p-XSC) is a more effective chemopreventive organoselenium compound and less toxic than benzyl selenocyanate (BSC) or the inorganic compound Na2SeO3. To explore mechanisms which mediate chemopreventive activities of p-XSC we have tested its effect on protein kinase A and C using in vitro and cell culture systems. While p-XSC did completely inhibit PKC and PKA activity, BSC was less active and Na2SeO3 had no effect. Comparative EC,, revealed values of 0.1, 1 and > 10 mu M for p-XSC, BSC and Na2SeO3, respectively. p-XSC was also capable of inhibiting protein phosphorylation in cultures of primary human fibroblasts and altered morphology of rat fibroblast (R6) cells. When combined, sub-optimal doses of p-XSC and staurosporine yielded an additive effect on cell morphology. The ability of p-XSC and BSC to inhibit protein kinase A and C activities may in part account for the mechanism(s) by which these agents mediate their chemopreventive effects.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.3892/ijo.7.3.685 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
The Role of Protein Kinase C During the Differentiation of Stem and Precursor Cells into Tissue Cells.
Biomedicines
November 2024
Department of Oral and Maxillofacial Surgery, University Hospital Regensburg, Franz-Josef-Strauss-Allee 11, 93053 Regensburg, Germany.
Protein kinase C (PKC) plays an essential role during many biological processes including development from early embryonic stages until the terminal differentiation of specialized cells. This review summarizes the current knowledge about the involvement of PKC in molecular processes during the differentiation of stem/precursor cells into tissue cells with a particular focus on osteogenic, adipogenic, chondrogenic and neuronal differentiation by using a comprehensive approach. Interestingly, studies examining the overall role of PKC, or one of its three isoform groups (classical, novel and atypical PKCs), often showed controversial results.
View Article and Find Full Text PDFRole of GPR55 receptor in bovine sperm capacitation.
Andrology
January 2025
Centro de Estudios Farmacológicos y Botánicos (CEFYBO), Facultad de Medicina-Universidad de Buenos Aires (UBA/CONICET), Buenos Aires, Argentina.
Background: Endocannabinoids like anandamide (AEA), among other lipids, are recognized signaling molecules that participate in reproductive events.
Objectives: Our aims were to characterize orphan G protein-coupled receptor (GPR55) presence; investigate GPR55 activation by AEA and determine GPR55 role in the bovine sperm function.
Materials And Methods: GPR55 presence was assessed by immunocytochemistry.
Oxygenase Ppo-Regulated Moldy Volatiles Affect Growth, Pathogenicity and Patulin Biosynthesis of Through G Protein Signaling.
J Fungi (Basel)
November 2024
College of Food Science and Engineering, Gansu Agricultural University, Lanzhou 730070, China.
Precocious sexual inducer (psi)-producing oxygenases (Ppos) participate in the production of C8 moldy volatile compounds (MVOCs), and these compounds could act as signal molecules modulating G protein signaling cascades, which participates in the growth and development, secondary metabolisms and pathogenicity of filamentous fungi. In this study, PePpoA and PePpoC proteins were identified in . The deletion of decreased C8 MVOC production in , while they were not detected in the strain ( < 0.
View Article and Find Full Text PDFSymptomatic Improvement in Adults and Adolescents with Eosinophilic Esophagitis Requires Higher Systemic Dupilumab Exposure than Histologic Response.
Clin Transl Gastroenterol
December 2024
Regeneron Pharmaceuticals Inc., Tarrytown, New York, USA.
Introduction: We assessed potential mechanisms behind the requirement for more frequent dupilumab dosing in eosinophilic esophagitis (EoE) compared with other approved indications.
Methods: Results for the phase 3 LIBERTY EoE TREET study co-primary endpoints (proportion of patients achieving a peak intraepithelial eosinophil count of ≤6 eosinophils per high-power field and absolute change from baseline in Dysphagia Symptom Questionnaire total score) were pooled in exposure-response analyses.
Results: A steep initial relationship then plateau was observed between higher dupilumab steady state trough concentrations (Ctrough) and decreased eosinophilic infiltration at Week 24, while a graded exposure-response relationship was observed for symptomatic improvement at Week 24.
Positive allosteric modulation of µ-opioid receptor - A new possible approach in the pain management?
Biochem Pharmacol
November 2024
Department of Biochemistry, Faculty of Medicine, Medical University of Lodz, Lodz, Poland. Electronic address:
The antinociceptive effect of the opioid drugs is achieved through activation of the µ-opioid receptor (MOP). The orthosteric and allosteric sites of opioid receptors may be modulated, orthosteric site by endogenous i.e.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!