Statins inhibit protein kinase D (PKD) activation in intestinal cells and prevent PKD1-induced growth of murine enteroids
We examined the impact of statins on protein kinase D (PKD) activation by G protein-coupled receptor (GPCR) agonists. Treatment of intestinal IEC-18 cells with cerivastatin inhibited PKD auto-phosphorylation at Ser916 induced by angiotensin II (ANG II) or vasopressin in a dose-dependent manner with half-maximal inhibition at 0.2 mM. Cerivastatin treatment inhibited PKD activation stimulated by these agonists for different times (5-60min) and blunted HDAC5 phosphorylation, a substrate of PKD. Other lipophilic statins, including simvastatin, atorvastatin and fluvastatin also prevented PKD activation in a dose-dependent manne...
Source: Am J Physiol Cell Ph... - February 13, 2023 Category: Cytology Authors: James Sinnett-Smith M Eugenia Torres-Marquez Jen-Kuan Chang Yuki Shimizu Fang Hao Martin G Martin Enrique Rozengurt Source Type: research
Statins inhibit protein kinase D (PKD) activation in intestinal cells and prevent PKD1-induced growth of murine enteroids
We examined the impact of statins on protein kinase D (PKD) activation by G protein-coupled receptor (GPCR) agonists. Treatment of intestinal IEC-18 cells with cerivastatin inhibited PKD auto-phosphorylation at Ser916 induced by angiotensin II (ANG II) or vasopressin in a dose-dependent manner with half-maximal inhibition at 0.2 mM. Cerivastatin treatment inhibited PKD activation stimulated by these agonists for different times (5-60min) and blunted HDAC5 phosphorylation, a substrate of PKD. Other lipophilic statins, including simvastatin, atorvastatin and fluvastatin also prevented PKD activation in a dose-dependent manne...
Source: American Journal of Physiology. Cell Physiology - February 13, 2023 Category: Cytology Authors: James Sinnett-Smith M Eugenia Torres-Marquez Jen-Kuan Chang Yuki Shimizu Fang Hao Martin G Martin Enrique Rozengurt Source Type: research
Statins inhibit protein kinase D (PKD) activation in intestinal cells and prevent PKD1-induced growth of murine enteroids
We examined the impact of statins on protein kinase D (PKD) activation by G protein-coupled receptor (GPCR) agonists. Treatment of intestinal IEC-18 cells with cerivastatin inhibited PKD auto-phosphorylation at Ser916 induced by angiotensin II (ANG II) or vasopressin in a dose-dependent manner with half-maximal inhibition at 0.2 mM. Cerivastatin treatment inhibited PKD activation stimulated by these agonists for different times (5-60min) and blunted HDAC5 phosphorylation, a substrate of PKD. Other lipophilic statins, including simvastatin, atorvastatin and fluvastatin also prevented PKD activation in a dose-dependent manne...
Source: Am J Physiol Cell Ph... - February 13, 2023 Category: Cytology Authors: James Sinnett-Smith M Eugenia Torres-Marquez Jen-Kuan Chang Yuki Shimizu Fang Hao Martin G Martin Enrique Rozengurt Source Type: research
Statins inhibit protein kinase D (PKD) activation in intestinal cells and prevent PKD1-induced growth of murine enteroids
We examined the impact of statins on protein kinase D (PKD) activation by G protein-coupled receptor (GPCR) agonists. Treatment of intestinal IEC-18 cells with cerivastatin inhibited PKD auto-phosphorylation at Ser916 induced by angiotensin II (ANG II) or vasopressin in a dose-dependent manner with half-maximal inhibition at 0.2 mM. Cerivastatin treatment inhibited PKD activation stimulated by these agonists for different times (5-60min) and blunted HDAC5 phosphorylation, a substrate of PKD. Other lipophilic statins, including simvastatin, atorvastatin and fluvastatin also prevented PKD activation in a dose-dependent manne...
Source: Am J Physiol Cell Ph... - February 13, 2023 Category: Cytology Authors: James Sinnett-Smith M Eugenia Torres-Marquez Jen-Kuan Chang Yuki Shimizu Fang Hao Martin G Martin Enrique Rozengurt Source Type: research
Statins inhibit protein kinase D (PKD) activation in intestinal cells and prevent PKD1-induced growth of murine enteroids
We examined the impact of statins on protein kinase D (PKD) activation by G protein-coupled receptor (GPCR) agonists. Treatment of intestinal IEC-18 cells with cerivastatin inhibited PKD auto-phosphorylation at Ser916 induced by angiotensin II (ANG II) or vasopressin in a dose-dependent manner with half-maximal inhibition at 0.2 mM. Cerivastatin treatment inhibited PKD activation stimulated by these agonists for different times (5-60min) and blunted HDAC5 phosphorylation, a substrate of PKD. Other lipophilic statins, including simvastatin, atorvastatin and fluvastatin also prevented PKD activation in a dose-dependent manne...
Source: American Journal of Physiology. Cell Physiology - February 13, 2023 Category: Cytology Authors: James Sinnett-Smith M Eugenia Torres-Marquez Jen-Kuan Chang Yuki Shimizu Fang Hao Martin G Martin Enrique Rozengurt Source Type: research
Statins inhibit protein kinase D (PKD) activation in intestinal cells and prevent PKD1-induced growth of murine enteroids
We examined the impact of statins on protein kinase D (PKD) activation by G protein-coupled receptor (GPCR) agonists. Treatment of intestinal IEC-18 cells with cerivastatin inhibited PKD auto-phosphorylation at Ser916 induced by angiotensin II (ANG II) or vasopressin in a dose-dependent manner with half-maximal inhibition at 0.2 mM. Cerivastatin treatment inhibited PKD activation stimulated by these agonists for different times (5-60min) and blunted HDAC5 phosphorylation, a substrate of PKD. Other lipophilic statins, including simvastatin, atorvastatin and fluvastatin also prevented PKD activation in a dose-dependent manne...
Source: American Journal of Physiology. Cell Physiology - February 13, 2023 Category: Cytology Authors: James Sinnett-Smith M Eugenia Torres-Marquez Jen-Kuan Chang Yuki Shimizu Fang Hao Martin G Martin Enrique Rozengurt Source Type: research
Statins inhibit protein kinase D (PKD) activation in intestinal cells and prevent PKD1-induced growth of murine enteroids
We examined the impact of statins on protein kinase D (PKD) activation by G protein-coupled receptor (GPCR) agonists. Treatment of intestinal IEC-18 cells with cerivastatin inhibited PKD auto-phosphorylation at Ser916 induced by angiotensin II (ANG II) or vasopressin in a dose-dependent manner with half-maximal inhibition at 0.2 mM. Cerivastatin treatment inhibited PKD activation stimulated by these agonists for different times (5-60min) and blunted HDAC5 phosphorylation, a substrate of PKD. Other lipophilic statins, including simvastatin, atorvastatin and fluvastatin also prevented PKD activation in a dose-dependent manne...
Source: Am J Physiol Cell Ph... - February 13, 2023 Category: Cytology Authors: James Sinnett-Smith M Eugenia Torres-Marquez Jen-Kuan Chang Yuki Shimizu Fang Hao Martin G Martin Enrique Rozengurt Source Type: research
Statins inhibit protein kinase D (PKD) activation in intestinal cells and prevent PKD1-induced growth of murine enteroids
We examined the impact of statins on protein kinase D (PKD) activation by G protein-coupled receptor (GPCR) agonists. Treatment of intestinal IEC-18 cells with cerivastatin inhibited PKD auto-phosphorylation at Ser916 induced by angiotensin II (ANG II) or vasopressin in a dose-dependent manner with half-maximal inhibition at 0.2 mM. Cerivastatin treatment inhibited PKD activation stimulated by these agonists for different times (5-60min) and blunted HDAC5 phosphorylation, a substrate of PKD. Other lipophilic statins, including simvastatin, atorvastatin and fluvastatin also prevented PKD activation in a dose-dependent manne...
Source: American Journal of Physiology. Cell Physiology - February 13, 2023 Category: Cytology Authors: James Sinnett-Smith M Eugenia Torres-Marquez Jen-Kuan Chang Yuki Shimizu Fang Hao Martin G Martin Enrique Rozengurt Source Type: research
Statins inhibit protein kinase D (PKD) activation in intestinal cells and prevent PKD1-induced growth of murine enteroids
We examined the impact of statins on protein kinase D (PKD) activation by G protein-coupled receptor (GPCR) agonists. Treatment of intestinal IEC-18 cells with cerivastatin inhibited PKD auto-phosphorylation at Ser916 induced by angiotensin II (ANG II) or vasopressin in a dose-dependent manner with half-maximal inhibition at 0.2 mM. Cerivastatin treatment inhibited PKD activation stimulated by these agonists for different times (5-60min) and blunted HDAC5 phosphorylation, a substrate of PKD. Other lipophilic statins, including simvastatin, atorvastatin and fluvastatin also prevented PKD activation in a dose-dependent manne...
Source: Am J Physiol Cell Ph... - February 13, 2023 Category: Cytology Authors: James Sinnett-Smith M Eugenia Torres-Marquez Jen-Kuan Chang Yuki Shimizu Fang Hao Martin G Martin Enrique Rozengurt Source Type: research
Statins inhibit protein kinase D (PKD) activation in intestinal cells and prevent PKD1-induced growth of murine enteroids
We examined the impact of statins on protein kinase D (PKD) activation by G protein-coupled receptor (GPCR) agonists. Treatment of intestinal IEC-18 cells with cerivastatin inhibited PKD auto-phosphorylation at Ser916 induced by angiotensin II (ANG II) or vasopressin in a dose-dependent manner with half-maximal inhibition at 0.2 mM. Cerivastatin treatment inhibited PKD activation stimulated by these agonists for different times (5-60min) and blunted HDAC5 phosphorylation, a substrate of PKD. Other lipophilic statins, including simvastatin, atorvastatin and fluvastatin also prevented PKD activation in a dose-dependent manne...
Source: American Journal of Physiology. Cell Physiology - February 13, 2023 Category: Cytology Authors: James Sinnett-Smith M Eugenia Torres-Marquez Jen-Kuan Chang Yuki Shimizu Fang Hao Martin G Martin Enrique Rozengurt Source Type: research
Statins inhibit protein kinase D (PKD) activation in intestinal cells and prevent PKD1-induced growth of murine enteroids
We examined the impact of statins on protein kinase D (PKD) activation by G protein-coupled receptor (GPCR) agonists. Treatment of intestinal IEC-18 cells with cerivastatin inhibited PKD auto-phosphorylation at Ser916 induced by angiotensin II (ANG II) or vasopressin in a dose-dependent manner with half-maximal inhibition at 0.2 mM. Cerivastatin treatment inhibited PKD activation stimulated by these agonists for different times (5-60min) and blunted HDAC5 phosphorylation, a substrate of PKD. Other lipophilic statins, including simvastatin, atorvastatin and fluvastatin also prevented PKD activation in a dose-dependent manne...
Source: Am J Physiol Cell Ph... - February 13, 2023 Category: Cytology Authors: James Sinnett-Smith M Eugenia Torres-Marquez Jen-Kuan Chang Yuki Shimizu Fang Hao Martin G Martin Enrique Rozengurt Source Type: research
High-throughput functional assay in cystic fibrosis patient-derived organoids allows drug repurposing
CONCLUSIONS: Future studies should focus on elucidating genotype specificity and mode-of-action of statins in more detail. This study exemplifies proof of principle of large-scale compound screening in a functional assay using patient-derived organoids.PMID:36726369 | PMC:PMC9885274 | DOI:10.1183/23120541.00495-2022 (Source: Cell Research)
Source: Cell Research - February 2, 2023 Category: Cytology Authors: Sacha Spelier Eyleen de Poel Georgia N Ithakisiou Sylvia W F Suen Marne C Hagemeijer Danya Muilwijk Annelotte M Vonk Jesse E Brunsveld Evelien Kruisselbrink Cornelis K van der Ent Jeffrey M Beekman Source Type: research
Induced pluripotent stem cell-derived cells model brain microvascular endothelial cell glucose metabolism
In this study, we examined differences between hpBMEC and hiBMEC glucose metabolism using a combination of dynamic metabolic measurements, metabolic mass spectrometry, RNA sequencing, and Western blots. hiBMEC had decrease d glycolytic flux relative to hpBMEC, and the overall metabolomes and metabolic enzyme levels were different between the two cell types. However, hpBMEC and hiBMEC had similar glucose metabolism, including nearly identical glucose labeled fractions of glycolytic and TCA cycle metabolites. Treatment with astrocyte conditioned media and high glucose increased glycolysis in both hpBMEC and hiBMEC, though hp...
Source: Fluids and Barriers of the CNS - December 9, 2022 Category: Neuroscience Source Type: research
[ASAP] Caffeic Acid-Grafted PLGA as a Novel Material for the Design of Fluvastatin-Eluting Nanoparticles for the Prevention of Neointimal Hyperplasia
Molecular PharmaceuticsDOI: 10.1021/acs.molpharmaceut.2c00693 (Source: Molecular Pharmaceutics)
Source: Molecular Pharmaceutics - October 17, 2022 Category: Drugs & Pharmacology Authors: Stefano Bellosta, Francesca Selmin, Giulia Magri, Silvia Castiglioni, Patrizia Procacci, Patrizia Sartori, Edoardo Scarpa, Valerio Tolva, Clara Rossi, Francesco Puoci, Loris Rizzello, and Francesco Cilurzo Source Type: research
GSE206635 SARS-CoV-2 disrupt respiratory vascular barrier by suppressing Claudin-5 expression (additional RNA-seq data)
In this study, we investigated the effect of SARS-CoV-2 on the endothelial barrier using an airway-on-a-chip that mimics respiratory organs and found that SARS-CoV-2 produced from infected epithelial cells disrupts the barrier by decreasing Claudin-5 (CLDN5), a tight junction protein, and disrupting vascular endothelial cadherin (VE-cadherin)-mediated adherens junctions. Consistently, the gene and protein expression levels of CLDN5 in a COVID-19 patient ’s lungs were decreased. CLDN5 overexpression or Fluvastatin treatment could rescue the SARS-CoV-2-induced respiratory endothelial barrier disruption. We therefore conclu...
Source: GEO: Gene Expression Omnibus - September 22, 2022 Category: Genetics & Stem Cells Tags: Expression profiling by high throughput sequencing Homo sapiens Source Type: research
