keyword
MENU ▼
Read by QxMD icon Read
search

Pi3kinase inhibitor

keyword
https://www.readbyqxmd.com/read/27762100/inhibition-of-dna-methyltransferases-regulates-cocaine-self-administration-by-rats-a-genome-wide-dna-methylation-study
#1
Mathieu Fonteneau, Dominique Filliol, Patrick Anglard, Katia Befort, Pascal Romieu, Jean Zwiller
DNA methylation is a major epigenetic process which regulates the accessibility of genes to the transcriptional machinery. In the present study, we investigated whether modifying the global DNA methylation pattern in the brain would alter cocaine intake by rats, using the cocaine self-administration test. The data indicate that treatment of rats with the DNA methyltransferase inhibitors 5-aza-2'-deoxycytidine and zebularine actually enhanced the reinforcing properties of cocaine. To get some insights about the underlying neurobiological mechanisms, a genome-wide methylation analysis was undertaken in the prefrontal cortex of rats self-administering cocaine and treated or not with 5-aza-2'-deoxycytidine...
October 20, 2016: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/26924019/endocannabinoid-2-ag-and-intracellular-cannabinoid-receptors-modulate-a-low-threshold-calcium-spike-induced-slow-depolarizing-afterpotential-in-rat-thalamic-paraventricular-nucleus-neurons
#2
L Zhang, M Kolaj, L P Renaud
In rat paraventricular thalamic nucleus (PVT) neurons, activation of low-threshold calcium (Ca(2+)) channels triggers a low-threshold spike (LTS) which may be followed by slow afterpotentials that can dramatically influence action potential patterning. Using gluconate-based internal recording solutions, we investigated the properties of a LTS-induced slow afterdepolarization (sADP) observed in a subpopulation of PVT neurons recorded in brain slice preparations. This LTS-induced sADP required T-type Ca(2+) channel opening, exhibited variable magnitudes between neurons and a voltage dependency with a maximum near -50 mV...
May 13, 2016: Neuroscience
https://www.readbyqxmd.com/read/26801880/inhibition-of-akt-enhances-the-chemopreventive-effects-of-topical-rapamycin-in-mouse-skin
#3
Sally E Dickinson, Jaroslav Janda, Jane Criswell, Karen Blohm-Mangone, Erik R Olson, Zhonglin Liu, Christy Barber, Emanuel F Petricoin, Valerie S Calvert, Janine Einspahr, Jesse E Dickinson, Steven P Stratton, Clara Curiel-Lewandrowski, Kathylynn Saboda, Chengcheng Hu, Ann M Bode, Zigang Dong, David S Alberts, G Timothy Bowden
The PI3Kinase/Akt/mTOR pathway has important roles in cancer development for multiple tumor types, including UV-induced nonmelanoma skin cancer. Immunosuppressed populations are at increased risk of aggressive cutaneous squamous cell carcinoma (SCC). Individuals who are treated with rapamycin (sirolimus, a classical mTOR inhibitor) have significantly decreased rates of developing new cutaneous SCCs compared with those that receive traditional immunosuppression. However, systemic rapamycin use can lead to significant adverse events...
March 2016: Cancer Prevention Research
https://www.readbyqxmd.com/read/26709648/gmp-grade-platelet-lysate-enhances-proliferation-and-migration-of-tenon-fibroblasts
#4
Augusto Carducci, Gaia Scafetta, Camilla Siciliano, Roberto Carnevale, Paolo Rosa, Andrea Coccia, Giorgio Mangino, Antonella Bordin, Enzo Maria Vingolo, Luca Pierelli, Eugenio Lendaro, Giuseppe Ragona, Giacomo Frati, Elena De Falco
Tenon's fibroblasts (TFs), widely employed as in vitro model for many ophthalmological studies, are routinely cultured with FBS. Platelet Lysate (PL), a hemoderivate enriched with growth factors and cytokines has been largely tested in several clinical applications and as substitute of FBS in culture. Here, we investigate whether PL can exert biological effects on TF populations similarly to other cell types. Results show that PL significantly enhances cell proliferation and migration vs. FBS, without influencing cell size/granularity...
2016: Frontiers in Bioscience (Elite Edition)
https://www.readbyqxmd.com/read/26470790/estrogen-mediated-inactivation-of-foxo3a-by-the-g-protein-coupled-estrogen-receptor-gper
#5
Erin Zekas, Eric R Prossnitz
BACKGROUND: Estrogen (17β-estradiol) promotes the survival and proliferation of breast cancer cells and its receptors represent important therapeutic targets. The cellular actions of estrogen are mediated by the nuclear estrogen receptors ERα and ERβ as well as the 7-transmembrane spanning G protein-coupled estrogen receptor (GPER). We previously reported that estrogen activates the phosphoinositide 3-kinase (PI3Kinase) pathway via GPER, resulting in phosphatidylinositol (3,4,5)-trisphosphate (PIP3) production within the nucleus of breast cancer cells; however, the mechanisms and consequences of this activity remained unclear...
October 15, 2015: BMC Cancer
https://www.readbyqxmd.com/read/26446173/regulation-of-b-type-natriuretic-peptide-synthesis-by-insulin-in-obesity-in-male-mice
#6
Haihua Zhang, Robrecht Thoonen, Vincent Yao, Emmanuel S Buys, John Popovich, Yan Ru Su, Thomas J Wang, Marielle Scherrer-Crosbie
Human studies suggest that insulin resistance and obesity are associated with a decrease in B-type natriuretic peptide (BNP) plasma concentrations. The objective of the study was to gain insights into the mechanisms involved in the association between insulin resistance and decreased BNP plasma concentrations. Mice fed a high-fat, high-fructose (HFHF) diet for 4 weeks developed mild obesity and systemic insulin resistance. Elevated plasma concentrations of insulin, glucose and triglycerides were noted. The HFHF diet was also associated with myocardial insulin resistance, characterized by an impaired response of the phosphoinositide 3-kinase-AKT (PI3K-AKT) pathway to insulin in the left ventricle...
January 2016: Experimental Physiology
https://www.readbyqxmd.com/read/26436560/zinc-pyrithione-inhibits-caspase-3-activity-promotes-erbb1-erbb2-heterodimerization-and-suppresses-erbb2-downregulation-in-cardiomyocytes-subjected-to-ischemia-reperfusion
#7
Vijaya Lakshmi Bodiga, Sandhya Thokala, Praveen Kumar Vemuri, Sreedhar Bodiga
Heart tissue becomes zinc-depleted and the capacity to mobilize labile zinc is diminished, indicating zinc dyshomeostasis during ischemia/reperfusion (I/R). Apparently, zinc pyrithione restores the basal zinc levels during I/R and prevents apoptosis by activating phosphatidyl inositol-3-kinase/Akt and targeting mitochondrial permeability transition. Receptor tyrosine kinases of the ErbB family (ErbB1 to ErbB4) are cell surface proteins that can regulate cell growth, proliferation and survival. Previous studies have shown that zinc pyrithione-induced activation of PI3kinase/Akt requires ErbB2 expression...
December 2015: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/26402163/a-short-report-pamm-a-novel-antioxidant-protein-induced-by-oxidative-stress
#8
Yan Xu, Leslie R Morse, Raquel Assed Bezerra da Silva, Dianhua Wang, Ricardo A Battaglino
Reactive oxygen species (ROS) play a central role in estrogen deficiency-induced bone loss. We previously identified and characterized a novel member of the Peroxiredoxin (PRX) like 2 family that we called PAMM: Peroxiredoxin Activated in M-CSF stimulated Monocytes, a redox regulatory protein that modulates osteoclast differentiation in vitro. In this study, we report increased PAMM expression in H2O2-treated cells and in bones from ovariectomized (OVX) mice 4 weeks after surgery, models for oxidative stress in vitro and in vivo, respectively...
December 2015: Redox Biology
https://www.readbyqxmd.com/read/26238638/identifying-molecular-targets-for-new-drug-development-for-chronic-obstructive-pulmonary-disease-what-does-the-future-hold
#9
REVIEW
Peter J Barnes
There is an urgent need to develop more effective therapies for chronic obstructive pulmonary disease (COPD) that target the underlying inflammatory disease process. Current therapies with long-acting bronchodilators and inhaled corticosteroids fail to prevent either disease progression or mortality, as they do not suppress the underlying inflammation. With better understanding of the inflammatory and destructive process in the pathophysiology of COPD, several new therapeutic targets have been identified. Several mediator antagonists or inhibitors tested in COPD have so far been disappointing...
August 2015: Seminars in Respiratory and Critical Care Medicine
https://www.readbyqxmd.com/read/25882870/involvement-of-smad2-and-erk-akt-cascade-in-tgf-%C3%AE-1-induced-apoptosis-in-human-gingival-epithelial-cells
#10
Tetsuya Yoshimoto, Tsuyoshi Fujita, Mikihito Kajiya, Shinji Matsuda, Kazuhisa Ouhara, Hideki Shiba, Hidemi Kurihara
Periodontitis is the most prevalent infectious disease caused by periodontopathic bacteria and is also a chronic inflammatory disease. Gingival crevicular fluid (GCF) is an inflammatory exudate that seeps into the gingival crevices or periodontal pockets around teeth with inflamed gingiva, and contains various materials including leukocytes and cytokines. Since gingival epithelial cells, which form a barrier against bacterial challenges, are affected by GCF, cytokines or other materials contained within GCF are engaged in the maintenance and disruption of the epithelial barrier...
September 2015: Cytokine
https://www.readbyqxmd.com/read/25878190/inhibition-of-the-phosphoinositide-3-kinase-pathway-for-the-treatment-of-patients-with-metastatic-metaplastic-breast-cancer
#11
S Moulder, T Helgason, F Janku, J Wheler, J Moroney, D Booser, C Albarracin, P K Morrow, J Atkins, K Koenig, M Gilcrease, R Kurzrock
BACKGROUND: Mesenchymal/metaplastic breast cancers (MpBCs) are often triple-negative (TNBC), and chemo-refractory, and can harbor phosphoinositide 3-kinase (PI3kinase) alterations; thus, therapy with mTor inhibitors may demonstrate activity. PATIENTS AND METHODS: Patients with mesenchymal/MpBC treated with temsirolimus-based regimens were evaluated. Mutational analyses [polymerase chain reaction (PCR)-based DNA sequencing method, mass spectrometric detection (Sequenom MassARRAY), or next-generation sequencing] as well as loss of phosphatase and tensin homolog (PTEN) (immunohistochemistry) were performed (archived tissue when available)...
July 2015: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/25051885/involvement-of-erk1-2-p38-mapk-and-pi3k-akt-signaling-pathways-in-the-regulation-of-cell-cycle-progression-by-pthrp-in-colon-adenocarcinoma-cells
#12
Natalia Calvo, María Julia Martín, Ana Russo de Boland, Claudia Gentili
Parathyroid hormone-related peptide (PTHrP) is distributed in most fetal and adult tissues, and its expression correlates with the severity of colon carcinoma. Recently we obtained evidence that in Caco-2 cells, a cell line from human colorectal adenocarcinoma, exogenous PTHrP increases the number of live cells, via ERK1/2, p38 MAPK, and PI3-kinase and induces the expression of cyclin D1, a cell cycle regulatory protein. In this study, we further investigated the role of PTHrP in the regulation of the cell cycle progression in these intestinal cells...
August 2014: Biochemistry and Cell Biology, Biochimie et Biologie Cellulaire
https://www.readbyqxmd.com/read/24530412/bdnf-mimetic-compound-lm22a-4-regulates-cementoblast-differentiation-via-the-trkb-erk-akt-signaling-cascade
#13
Mikihito Kajiya, Kei Takeshita, Mizuho Kittaka, Shinji Matsuda, Kazuhisa Ouhara, Katsuhiro Takeda, Takashi Takata, Masae Kitagawa, Tsuyoshi Fujita, Hideki Shiba, Hidemi Kurihara
Brain-derived neurotrophic factor (BDNF) activates its receptor TrkB, and promotes neuronal survival, differentiation, and synaptic functions. Furthermore, we have revealed that BDNF can also regulate cementoblast differentiation and cellular survival via TrkB-ERK/Akt signaling cascade, which, in turn, results in the induction of periodontal tissue regeneration. Recently, using in silico screening with a BDNF loop-domain pharmacophore, a small molecule BDNF mimetic, called LM22A-4 that can facilitate TrkB signaling in hippocampal neurons to prevent cell death, was identified...
April 2014: International Immunopharmacology
https://www.readbyqxmd.com/read/24155894/natriuretic-peptide-receptor-c-agonist-attenuates-the-expression-of-cell-cycle-proteins-and-proliferation-of-vascular-smooth-muscle-cells-from-spontaneously-hypertensive-rats-role-of-gi-proteins-and-mapkinase-pi3kinase-signaling
#14
Jasmine El Andalousi, Yuan Li, Madhu B Anand-Srivastava
Vascular smooth muscle cells (VSMC) from spontaneously hypertensive rats (SHR) exhibit hyperproliferation and overexpression of cell cycle proteins. We earlier showed that small peptide fragments of cytoplasmic domain of natriuretic receptor-C (NPR-C) attenuate vasoactive peptide-induced hyperproliferation of VSMC. The present study investigated if C-ANP4-23, a specific agonist of NPR-C, could attanuate the hyperproliferation of VSMC from SHR by inhibiting the overexpression of cell cycle proteins and examine the underlying signaling pathways contributing to this inhibition...
2013: PloS One
https://www.readbyqxmd.com/read/23711177/ephb-and-ephrin-b-interactions-mediate-human-mesenchymal-stem-cell-suppression-of-activated-t-cells
#15
Thao M Nguyen, Agnes Arthur, John D Hayball, Stan Gronthos
Mesenchymal stromal/stem cells (MSC) express the contact-dependent erythropoietin-producing hepatocellular (Eph) receptor tyrosine kinase family and their cognate ephrin ligands, which are known to regulate thymocyte maturation and selection, T-cell transendothelial migration, activation, co-stimulation, and proliferation. However, the contribution of Eph/ephrin molecules in mediating human MSC suppression of activated T-cells remains to be determined. In the present study, we showed that EphB2 and ephrin-B2 are expressed by ex vivo expanded MSC, while the corresponding ligands, ephrin-B1 and EphB4, respectively, are highly expressed by T-cells...
October 15, 2013: Stem Cells and Development
https://www.readbyqxmd.com/read/23705826/cell-cycle-dependent-activity-of-the-novel-dual-pi3k-mtorc1-2-inhibitor-nvp-bgt226-in-acute-leukemia
#16
Kerstin Maria Kampa-Schittenhelm, Michael Charles Heinrich, Figen Akmut, Katharina Henriette Rasp, Barbara Illing, Hartmut Döhner, Konstanze Döhner, Marcus Matthias Schittenhelm
BACKGROUND: Dysregulation of the PI3Kinase/AKT pathway is involved in the pathogenesis of many human malignancies. In acute leukemia, the AKT pathway is frequently activated, however mutations in the PI3K/AKT pathway are uncommon. In some cases, constitutive AKT activation can be linked to gain-of-function tyrosine kinase (TK) mutations upstream of the PI3K/AKT pathway. Inhibitors of the PI3K/AKT pathway are attractive candidates for cancer drug development, but so far clinical efficacy of PI3K inhibitors against various neoplasms has been moderate...
2013: Molecular Cancer
https://www.readbyqxmd.com/read/23626723/an-alkylphenol-mix-promotes-seminoma-derived-cell-proliferation-through-an-eralpha36-mediated-mechanism
#17
Hussein Ajj, Amand Chesnel, Sophie Pinel, François Plenat, Stephane Flament, Helene Dumond
Long chain alkylphenols are man-made compounds still present in industrial and agricultural processes. Their main use is domestic and they are widespread in household products, cleansers and cosmetics, leading to a global environmental and human contamination. These molecules are known to exert estrogen-like activities through binding to classical estrogen receptors. In vitro, they can also interact with the G-protein coupled estrogen receptor. Testicular germ cell tumor etiology and progression are proposed to be stimulated by lifelong estrogeno-mimetic exposure...
2013: PloS One
https://www.readbyqxmd.com/read/23592328/akt-regulates-glutamate-receptor-trafficking-and-postsynaptic-membrane-elaboration-at-the-drosophila-neuromuscular-junction
#18
Hyun-Gwan Lee, Na Zhao, Bridget K Campion, Michelle M Nguyen, Scott B Selleck
The Akt family of serine-threonine kinases integrates a myriad of signals governing cell proliferation, apoptosis, glucose metabolism, and cytoskeletal organization. Akt affects neuronal morphology and function, influencing dendrite growth and the expression of ion channels. Akt is also an integral element of PI3Kinase-target of rapamycin (TOR)-Rheb signaling, a pathway that affects synapse assembly in both vertebrates and Drosophila. Our recent findings demonstrated that disruption of this pathway in Drosophila is responsible for a number of neurodevelopmental deficits that may also affect phenotypes associated with tuberous sclerosis complex, a disorder resulting from mutations compromising the TSC1/TSC2 complex, an inhibitor of TOR (Dimitroff et al...
October 2013: Developmental Neurobiology
https://www.readbyqxmd.com/read/23522913/combined-inhibition-of-the-phosphoinosityl-3-kinase-pi3kinase-p110%C3%AE-subunit-and-mitogen-extracellular-activated-protein-kinase-mekinase-shows-synergistic-cytotoxicity-against-human-acute-myeloid-leukemia-progenitors
#19
Yan Xing, Donna E Hogge
Treatment of 32 acute myeloid leukemia (AML) blast samples showing activation of the PI3K and RAS/RAF/MEK/ERK pathways with the PI3K p110δ isoform and MEKinase selective inhibitors, PCN5603 and U0126 produced dose dependent progenitor kill and inhibition of p-Akt Ser473 and p-Erk Tyr204 expression. Normal marrow or blood progenitors were less sensitive to these inhibitors (median PCN5603 IC₅₀s for AML and normal cells 1.5 and 5.8 μM and for U0126 9.6 and 25.8 μM, respectively). U0126 synergized with PCN5603 for killing of both AML and normal progenitors...
June 2013: Leukemia Research
https://www.readbyqxmd.com/read/23328930/resveratrol-inhibits-tnf-%C3%AE-induced-il-1%C3%AE-mmp-3-production-in-human-rheumatoid-arthritis-fibroblast-like-synoviocytes-via-modulation-of-pi3kinase-akt-pathway
#20
Jing Tian, Jin-wei Chen, Jie-sheng Gao, Len Li, Xi Xie
Resveratrol (trans-3,4'-trihydroxystilbene), a natural phytoalexin, possesses anti-inflammatory, anti-proliferative, and immunomodulatory properties and has the potential for treating inflammatory disorders. The present study was designed to investigate the effects of resveratrol on TNF-α-induced inflammatory cytokines production of IL-1β and MMP3 in Rheumatoid arthritis (RA) Fibroblast-like synoviocytes (FLS) and further to explore the role of PI3K/Akt signaling pathway by which resveratrol modulates those cytokines production...
July 2013: Rheumatology International
keyword
keyword
81350
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"