keyword
MENU ▼
Read by QxMD icon Read
search

forskolin

keyword
https://www.readbyqxmd.com/read/28223412/identification-of-a-selective-small-molecule-inhibitor-of-type-1-adenylyl-cyclase-activity-with-analgesic-properties
#1
Tarsis F Brust, Doungkamol Alongkronrusmee, Monica Soto-Velasquez, Tanya A Baldwin, Zhishi Ye, Mingji Dai, Carmen W Dessauer, Richard M van Rijn, Val J Watts
Adenylyl cyclase 1 (AC1) belongs to a group of adenylyl cyclases (ACs) that are stimulated by calcium in a calmodulin-dependent manner. Studies with AC1 knockout mice suggest that inhibitors of AC1 may be useful for treating pain and opioid dependence. However, nonselective inhibition of AC isoforms could result in substantial adverse effects. We used chemical library screening to identify a selective AC1 inhibitor with a chromone core structure that may represent a new analgesic agent. After demonstrating that the compound (ST034307) inhibited Ca(2+)-stimulated adenosine 3',5'-monophosphate (cAMP) accumulation in human embryonic kidney (HEK) cells stably transfected with AC1 (HEK-AC1 cells), we confirmed selectivity for AC1 by testing against all isoforms of membrane-bound ACs...
February 21, 2017: Science Signaling
https://www.readbyqxmd.com/read/28222855/direct-growth-inhibitory-effects-of-prostaglandin-e2-in%C3%A2-pancreatic-cancer-cells-in%C3%A2-vitro-through-an-ep4-pka-mediated-mechanism
#2
Andrea Schmidt, James Sinnett-Smith, Steven Young, Hui-Hua Chang, O Joe Hines, David W Dawson, Enrique Rozengurt, Guido Eibl
BACKGROUND: There is strong evidence linking inflammation and the development of pancreatic ductal adenocarcinoma. Cyclooxygenase-2 (COX-2) and COX-2-derived PGE2 are overexpressed in human and murine pancreatic ductal adenocarcinoma. Several studies have demonstrated an important role of COX-2-derived PGE2 in tumor-stroma interactions; however, the direct growth effects of prostaglandin E2 (PGE2) on pancreatic ductal adenocarcinoma cells is less well defined. Our aim was to investigate the effects of PGE2 on pancreatic ductal adenocarcinoma cell growth and to characterize the underlying mechanisms...
February 17, 2017: Surgery
https://www.readbyqxmd.com/read/28216156/epac-mediates-camp-induced-proliferation-of-rat-anterior-pituitary-gh3-cells-via-the-activation-of-extracellular-signal-regulated-kinase
#3
Wei Sun, Wei Jiao, Yimin Huang, Ran Li, Zhuo Zhang, Junwen Wang, Ting Lei
Cyclic adenosine 3'-5'-monophosphate (cAMP) plays a crucial role in regulating pituitary cell proliferation and hormone synthesis. Recent evidence suggests that exchange proteins directly activated by cAMP (Epacs) may mediate the effects of cAMP. Here we used rat anterior pituitary GH3 cells as the experiment model to demonstrate that forskolin increased the proliferation of GH3 cells and the phosphorylation of ERK1/2, and these effects were inhibited by PKA or Epac inhibitors. Epac activator 8-pCPT-2'-O-Me-cAMP increased GH3 cell proliferation and this was blocked by ESI-09, an Epac inhibitor...
February 16, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28215673/supplement-of-cilostamide-in-growth-medium-improves-oocyte-maturation-and-developmental-competence-of-embryos-derived-from-small-antral-follicles-in-pigs
#4
Hanna Lee, Fazle Elahi, Joohyeong Lee, Seung Tae Lee, Sang-Hwan Hyun, Eunsong Lee
This study was conducted to evaluate the effects of cyclic AMP (cAMP) modulator cilostamide (CIL) and forskolin (FSK) treatment during in vitro growth (IVG) on growth, maturation, and embryonic development of cumulus-oocyte complexes (COCs) derived from small antral follicles < 3 mm in diameter (SAFCOCs). SAFCOCs were untreated (control) or treated with 20 μM CIL and/or 50 μM FSK for 2 days for IVG. Next, IVG oocytes were cultured for maturation and then induced for parthenogenesis (PA) or used as recipient ooplasts for somatic cell nuclear transfer (SCNT)...
March 15, 2017: Theriogenology
https://www.readbyqxmd.com/read/28213516/rapid-regulation-of-sialidase-activity-in-response-to-neural-activity-and-sialic-acid-removal-during-memory-processing-in-rat-hippocampus
#5
Akira Minami, Yuko Meguro, Sayaka Ishibashi, Ami Ishii, Mako Shiratori, Saki Sai, Yuuki Horii, Hirotaka Shimizu, Hokuto Fukumoto, Sumika Shinba, Risa Taguchi, Tadanobu Takahashi, Tadamune Otsubo, Kiyoshi Ikeda, Takashi Suzuki
Sialidase cleaves sialic acids on the extracellular cell surface as well as inside the cell, and is necessary for normal long-term potentiation (LTP) at MF-CA3 pyramidal cell synapses and for hippocampus-dependent spatial memory. Here, we investigated in detail the role of sialidase in memory processing. Sialidase activity measured with 4MU-Neu5Ac or X-Neu5Ac and FRV LB was increased by high K(+)-induced membrane depolarization. Sialidase activity was also increased by chemical LTP induction with forskolin and activation of BDNF signaling, non-NMDARs or NMDARs...
February 17, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28196531/enhancing-circadian-clock-function-in-cancer-cells-inhibits-tumor-growth
#6
Silke Kiessling, Lou Beaulieu-Laroche, Ian D Blum, Dominic Landgraf, David K Welsh, Kai-Florian Storch, Nathalie Labrecque, Nicolas Cermakian
BACKGROUND: Circadian clocks control cell cycle factors, and circadian disruption promotes cancer. To address whether enhancing circadian rhythmicity in tumor cells affects cell cycle progression and reduces proliferation, we compared growth and cell cycle events of B16 melanoma cells and tumors with either a functional or dysfunctional clock. RESULTS: We found that clock genes were suppressed in B16 cells and tumors, but treatments inducing circadian rhythmicity, such as dexamethasone, forskolin and heat shock, triggered rhythmic clock and cell cycle gene expression, which resulted in fewer cells in S phase and more in G1 phase...
February 14, 2017: BMC Biology
https://www.readbyqxmd.com/read/28179537/early-tyrosine-phosphorylation-events-following-adenosine-a2a-receptor-in-human-neutrophils-identification-of-regulated-pathways
#7
Miriam S Giambelluca, Marc Pouliot
Activation of the adenosine 2A receptor (A2AR) elevates intracellular levels of cAMP and acts as a physiologic inhibitor of inflammatory neutrophil functions. In this study, we looked into the impact of A2AR engagement on early phosphorylation events. Neutrophils were stimulated with well-characterized proinflammatory agonists in the absence or presence of an A2AR agonist {3-[4-[2-[ [6-amino-9-[(2R,3R,4S,5S)-5-(ethylcarbamoyl)-3,4-dihydroxy-oxolan-2-yl]purin-2-yl]amino] ethyl] phenyl] propanoic acid (CGS 21680)}, PGE2, or a mixture of the compounds RO 20-1724 and forskolin...
February 8, 2017: Journal of Leukocyte Biology
https://www.readbyqxmd.com/read/28179449/the-gip-gipr-axis-is-functionally-linked-to-gh-secretion-increase-in-a-significant-proportion-of-gsp-somatotropinomas
#8
Daniela Regazzo, Marco Losa, Nora Albiger, Maria Rosa Terreni, Giovanni Vazza, Filippo Ceccato, Enzo Emanuelli, Luca Denaro, Carla Scaroni, Gianluca Occhi
Objective: Glucose-dependent insulinotropic polypeptide receptor (GIPR) overexpression has been recently described in a proportion of gsp(-) somatotropinomas and suggested to be associated with the paradoxical increase of GH (GH-PI) during an oral glucose load. Design and Methods: This study was aimed at linking the GIP/GIPR pathway to GH secretion in 25 somatotropinomas-derived primary cultures and correlating molecular with clinical features in acromegalic patients. Given the impairment of the GIPR/GIPR axis in acromegaly, an additional aim was to assess the effect of GH/IGF-1 stimulation on GIP expression in the enteroendocrine cell line STC-1...
February 8, 2017: European Journal of Endocrinology
https://www.readbyqxmd.com/read/28177982/pharmacological-activation-of-protein-kinase-a-improves-memory-loss-and-neuropathological-changes-in-a-mouse-model-of-dementia-of-alzheimer-s-type
#9
Amit Kumar, Nirmal Singh
The study investigates the therapeutic potential of the protein kinase A (PKA) activator forskolin in cognitive deficits of mice. Streptozotocin (STZ) [3 mg/kg, intracerebroventricularly (i.c.v.)] was used to induce memory deficits in mice, whereas aged mice served as natural model of dementia. Forskolin (2.5, 5, and 10 mg/kg/day, oral) treatment was administered to i.c.v. STZ-treated and aged mice for 14 days. The Morris Water Maze test was used to evaluate learning and memory. Estimation of brain acetylcholinesterase (AChE) activity, brain glutathione, thiobarbituric acid-reactive species, brain myeloperoxidase levels, and histopathological studies were also performed...
February 7, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28161254/pharmacological-inhibition-of-dna-methyltransferase-1-promotes-neuronal-differentiation-from-rodent-and-human-nasal-olfactory-stem-progenitor-cell-cultures
#10
I Franco, L Ortiz-López, B Roque-Ramírez, G B Ramírez-Rodríguez, M Lamas
Nasal olfactory stem and neural progenitor cells (NOS/PCs) are considered possible tools for regenerative stem cell therapies in neurodegenerative diseases. Neurogenesis is a complex process regulated by extrinsic and intrinsic signals that include DNA-methylation and other chromatin modifications that could be experimentally manipulated in order to increase neuronal differentiation. The aim of the present study was the characterization of primary cultures and consecutive passages (P2-P10) of NOS/PCs isolated from male Swiss-Webster (mNOS/PCs) or healthy humans (hNOS/PCs)...
February 1, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28157484/small-molecules-modulate-chromatin-accessibility-to-promote-neurog2-mediated-fibroblast-to-neuron-reprogramming
#11
Derek K Smith, Jianjing Yang, Meng-Lu Liu, Chun-Li Zhang
Pro-neural transcription factors and small molecules can induce the reprogramming of fibroblasts into functional neurons; however, the immediate-early molecular events that catalyze this conversion have not been well defined. We previously demonstrated that neurogenin 2 (NEUROG2), forskolin (F), and dorsomorphin (D) can reprogram fibroblasts into functional neurons with high efficiency. Here, we used this model to define the genetic and epigenetic events that initiate an acquisition of neuronal identity. We demonstrate that NEUROG2 is a pioneer factor, FD enhances chromatin accessibility and H3K27 acetylation, and synergistic transcription activated by these factors is essential to successful reprogramming...
November 8, 2016: Stem Cell Reports
https://www.readbyqxmd.com/read/28133948/maternal-high-salt-diet-altered-adenosine-mediated-vasodilatation-via-pka-bkchannel-pathway-in-offspring-rats
#12
Jue Wu, Na Li, Yanping Liu, Weisheng Li, Axin He, Di Zhu, Xueqin Feng, Bailin Liu, Ruixiu Shi, Yujuan Zhang, Juanxiu Lv, Zhice Xu
SCOPE: High salt (HS) diets are related to cardiovascular diseases, and prenatal HS was suggested to increase risks of coronary artery diseases in the offspring. This study tested the hypothesis that prenatal HS may influence Adenosine-induced vasodilatation via PKA pathway in coronary arteries. METHODS AND RESULTS: Sprague-Dawley rats were fed with 8% salt diet for gestation, the control was fed with 0.3% salt diet. Coronary arteries from male adult offspring were tested for K(+) channels and Adenosine signal pathways...
January 29, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/28129894/reporter-cell-lines-for-detection-of-pertussis-toxin-in-acellular-pertussis-vaccines-as-a-functional-animal-free-alternative-to-the-in-vivo-histamine-sensitization-test
#13
Marieke E Hoonakker, Lisa M Verhagen, Larissa van der Maas, Arjen Sloots, Coenraad F M Hendriksen
Detoxified pertussis toxin (pertussis toxoid) is a major antigen in acellular pertussis vaccines. Testing these vaccines on the presence of residual pertussis toxin (PTx) and reversion to toxicity is performed by the regulatory required in vivo Histamine Sensitization test (HIST). Lack of mechanistic understanding of the HIST, technical handicaps and animal welfare concerns, have promoted the development of alternative methods. As the majority of the cellular effects of PTx depend on its ability to activate intracellular pathways involving cAMP, the in vitro cAMP-PTx assay was developed...
January 24, 2017: Vaccine
https://www.readbyqxmd.com/read/28126833/ghrelin-induces-clock-gene-expression-in-the-liver-of-goldfish-in-vitro-via-protein-kinase-c-and-protein-kinase-a-pathways
#14
Aída Sánchez-Bretaño, Ayelén M Blanco, Ángel L Alonso-Gómez, María J Delgado, Olivier Kah, Esther Isorna
The liver is the most important link between the circadian system and metabolism. As a food entrainable oscillator, the hepatic clock needs to be entrained by food-related signals. The objective of the present study was to investigate the possible role of ghrelin (an orexigenic peptide mainly synthesized in the gastrointestinal tract) as an endogenous synchronizer of the liver oscillator in teleosts. To achieve this aim, we first examined the presence of ghrelin receptors in the liver of goldfish. Then, the ghrelin regulation of clock gene expression in the goldfish liver was studied...
January 26, 2017: Journal of Experimental Biology
https://www.readbyqxmd.com/read/28126588/the-naturally-occurring-mutation-y197c-does-not-affect-the-expression-or-signaling-of-the-human-histamine-h3-receptor
#15
Cecilia Flores-Clemente, Juan Escamilla-Sánchez, Juan-Manuel Arias, José-Antonio Arias-Montaño
There is evidence for genetic polymorphism within the human histamine H3 receptor (hH3R), and a Tyr to Cys exchange at position 197 (Y197C), located in the amino terminus of the fifth transmembrane domain, has been reported. In this work we compared the expression and the pharmacological and signaling properties of wild-type (hH3RWT) and mutant (hH3RY197C) receptors transiently expressed in CHO-K1 cells. The hH3RY197C cDNA was created by overlap extension PCR amplification. Receptor expression and affinity were assessed by N-α-[methyl-(3)H]-histamine binding to cell membranes and intact cells...
January 23, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28124089/evening-primrose-oil-or-forskolin-ameliorates-celecoxib-enhanced-upregulation-of-tissue-factor-expression-in-mice-subjected-to-lipopolysaccharide-induced-endotoxemia
#16
Sarah M Mosaad, Sawsan A Zaitone, Amal A M Ahmed, Dina M Abo-Elmatty, Amani A El-Baz, Yasser M Moustafa
Celecoxib, a selective cyclooxygenase-2 inhibitor, produces thrombotic events in patients predisposed to cardiovascular risk factors. One theory reported an increase in endothelial expression of tissue factor (TF) as a predisposing factor. This work explored the effect of evening primrose oil (EPO), a source of prostaglandin E1, and forskolin (a cyclic adenosine monophosphate stimulator) against the prothrombotic effect of celecoxib in mice. Lipopolysaccharide mouse model of endotoxemia was used to induce an upregulation of TF activity...
January 26, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28106114/multiplexing-pka-and-erk1-2-kinases-fret-biosensors-in-living-cells-using-single-excitation-wavelength-dual-colour-flim
#17
Claire Demeautis, François Sipieter, Julien Roul, Catherine Chapuis, Sergi Padilla-Parra, Franck B Riquet, Marc Tramier
Monitoring of different signalling enzymes in a single assay using multiplex biosensing provides a multidimensional workspace to elucidate biological processes, signalling pathway crosstalk, and determine precise sequence of events at the single living cell level. In this study, we interrogate the complexity in cAMP/PKA-MAPK/ERK1&2 crosstalk by using multi-parameter biosensing experiments to correlate biochemical activities simultaneously in time and space. Using a single excitation wavelength dual colour FLIM method we are able to detect fluorescence lifetime images of two donors to simultaneously measure PKA and ERK1&2 kinase activities in the same cellular localization by using FRET biosensors...
January 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28103136/inhibition-of-voltage-dependent-potassium-channels-mediates-camp-potentiated-insulin-secretion-in-rat-pancreatic-%C3%AE-cells
#18
Yunfeng Liu, Xiangqin Zhong, Yaqin Ding, Lele Ren, Tao Bai, Mengmeng Liu, Zhihong Liu, Yangyan Guo, Qing Guo, Yu Zhang, Jing Yang, Yi Zhang
Insulin secretion is essential for maintenance of glucose homeostasis. An important intracellular signal regulating insulin secretion is cAMP. In this report, we showed that an increase of cAMP induced by adenylyl cyclase (AC) activator forskolin or by cAMP analog db-cAMP not only potentiated insulin secretion but also inhibited Kv channels, and these effects were reversed by AC inhibitor SQ22536. The cAMP-mediated Kv channel inhibition resulted in prolongation of action potential duration, which partly accounts for the elevation of intracellular Ca(2+) induced by activation of cAMP signaling...
January 19, 2017: Islets
https://www.readbyqxmd.com/read/28076805/regulation-of-active-icam-4-on-normal-and-sickle-cell-disease-rbcs-via-akaps-is-revealed-by-afm
#19
Jing Zhang, Krithika Abiraman, Sasia-Marie Jones, George Lykotrafitis, Biree Andemariam
Human healthy (wild-type (WT)) and homozygous sickle (SS) red blood cells (RBCs) express a large number of surface receptors that mediate cell adhesion between RBCs, and between RBCs and white blood cells, platelets, and the endothelium. In sickle cell disease (SCD), abnormal adhesion of RBCs to endothelial cells is mediated by the intercellular adhesion molecule-4 (ICAM-4), which appears on the RBC membrane and binds to the endothelial αvβ3 integrin. This is a key factor in the initiation of vaso-occlusive episodes, the hallmark of SCD...
January 10, 2017: Biophysical Journal
https://www.readbyqxmd.com/read/28063130/glucocorticoids-curtail-stimuli-induced-creb-phosphorylation-in-trh-neurons-through-interaction-of-the-glucocorticoid-receptor-with-the-catalytic-subunit-of-protein-kinase-a
#20
Israim Sotelo-Rivera, Antonieta Cote-Vélez, Rosa-María Uribe, Jean-Louis Charli, Patricia Joseph-Bravo
PURPOSE: Corticosterone prevents cold-induced stimulation of thyrotropin-releasing hormone (Trh) expression in rats, and the stimulatory effect of dibutyryl cyclic-adenosine monophosphate (dB-cAMP) on Trh transcription in hypothalamic cultures. We searched for the mechanism of this interference. METHODS: Immunohistochemical analyses of phosphorylated cAMP-response element binding protein (pCREB) were performed in the paraventricular nucleus (PVN) of Wistar rats, and in cell cultures of 17-day old rat hypothalami, or neuroblastoma SH-SY5Y cells...
January 6, 2017: Endocrine
keyword
keyword
37253
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"