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https://www.readbyqxmd.com/read/28636912/channeling-of-camp-in-pde-pka-complexes-promotes-signal-adaptation
#1
Nikhil Kumar Tulsian, Srinath Krishnamurthy, Ganesh Srinivasan Anand
Spatiotemporal control of the cAMP signaling pathway is governed by both hormonal stimulation of cAMP generation by adenylyl cyclases (activation phase) and cAMP hydrolysis by phosphodiesterases (PDEs) (termination phase). The termination phase is initiated by PDEs actively targeting the protein kinase A (PKA) R-subunit through formation of a PDE-PKAR-cyclic adenosine monophosphate (cAMP) complex (the termination complex). Our results using PDE8 as a model PDE, reveal that PDEs mediate active hydrolysis of cAMP bound to its receptor RIα by enhancing the enzymatic activity...
June 20, 2017: Biophysical Journal
https://www.readbyqxmd.com/read/28634298/analyses-of-pde-regulated-phosphoproteomes-reveal-unique-and-specific-camp-signaling-modules-in-t-cells
#2
Michael-Claude G Beltejar, Ho-Tak Lau, Martin G Golkowski, Shao-En Ong, Joseph A Beavo
Specific functions for different cyclic nucleotide phosphodiesterases (PDEs) have not yet been identified in most cell types. Conventional approaches to study PDE function typically rely on measurements of global cAMP, general increases in cAMP-dependent protein kinase (PKA), or the activity of exchange protein activated by cAMP (EPAC). Although newer approaches using subcellularly targeted FRET reporter sensors have helped define more compartmentalized regulation of cAMP, PKA, and EPAC, they have limited ability to link this regulation to downstream effector molecules and biological functions...
June 20, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28618988/synthesis-docking-and-anti-inflammatory-activity-of-triazole-amine-derivatives-as-potential-phosphodiesterase-4-inhibitors
#3
Ajmer Singh Grewal, Viney Lather, Deepti Pandita, Ruchi Dalal
BACKGROUND: Phosphodiesterase 4 (PDE4), one of the member of PDE superfamily catalyzes, the hydrolysis of cyclic adenosine monophosphate to adenosine monophosphate in pro-inflammatory and immunomodulatory cells leading to increased inflammatory processes. PDE4 has been reported as an attractive therapeutic target involved in various inflammatory disorders. OBJECTIVE: The present work was designed to synthesize and evaluate the anti-inflammatory activity of some new triazole amine derivatives as potential PDE4 inhibitors...
June 16, 2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28613871/discovery-of-n-4-5-4-fluoro-phenyl-3-methyl-2-methylsulfanyl-3h-imidazol-4-yl-pyridin-2-yl-acetamide-cbs-3595-a-dual-p38%C3%AE-mapk-pde-4-inhibitor-with-activity-against-tnf%C3%AE-related-diseases
#4
Wolfgang Albrecht, Anke Unger, Silke M Bauer, Stefan A Laufer
The anti-inflammatory potential of p38 mitogen-activated protein kinase (MAPK) inhibitors was coincidentally expanded to a dual inhibition of p38α MAPK and phosphodiesterase 4 (PDE4) and the potential benefits arising from the blockage of both inflammation-related enzymes were thoroughly investigated. The most promising compound, CBS-3595 (1), was successively evaluated in in vitro experiments as well as in ex vivo and in vivo preclinical studies after administration of 1 to rodents, dogs and monkeys. The resulting data clearly indicated a potent suppression of tumor necrosis factor alpha (TNFα) release...
June 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28603044/relaxation-of-isolated-guinea-pig-trachea-by-apigenin-a-constituent-of-celery-via-inhibition-of-phosphodiesterase
#5
Junn-Lain Chen, Wun-Chang Ko
Apigenin, was reported to have vasodilatory effects by inhibiting Ca(2+) influx through both voltage- and receptor-operated calcium channels, but not by inhibiting cAMP- or cGMP-phosphodiesterases (PDEs) in rat thoracic aorta. However, apigenin was reported to inhibit PDE1, 2 and 3 in guinea-pig lung and heart. The aim of this study was to clarify that guinea-pig tracheal relaxation by apigenin whether via PDE inhibition. We isometrically recorded the tension of isolated guinea-pig tracheal segments on a polygraph...
June 9, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28597753/circulatory-power-and-ventilatory-power-over-time-under-goal-oriented-sequential-combination-therapy-for-pulmonary-arterial-hypertension
#6
Akihiro Hirashiki, Shiro Adachi, Yoshihisa Nakano, Yoshihiro Kamimura, Shigetake Shimokata, Kyosuke Takeshita, Atsuya Shimizu, Kenji Toba, Toyoaki Murohara, Takahisa Kondo
Many therapeutic options are available for patients with pulmonary arterial hypertension (PAH). However, little is known about the effects of sequential combination therapy on exercise capacity. Here we monitored exercise capacity by cardiopulmonary exercise testing (CPX) and observed the benefit of using a peak VO2 cutoff of 15 mL/kg/min to guide combination therapy. Thirty patients newly diagnosed with PAH were treated with goal-oriented sequential combination therapy. Endothelin receptor antagonists (ERA) were the first-line treatment, with phosphodiesterase type 5 inhibitors (PDE-5i) as the preferred combination partner...
April 2017: Pulmonary Circulation
https://www.readbyqxmd.com/read/28594924/multiple-extracellular-vesicle-types-in-peritoneal-dialysis-effluent-are-prominent-and-contain-known-biomarkers
#7
Lachlan James Pearson, I-Yanut Klaharn, Bussakorn Thongsawang, Wasin Manuprasert, Thunvarat Saejew, Poorichaya Somparn, Piyatida Chuengsaman, Talerngsak Kanjanabuch, Trairak Pisitkun
Peritoneal dialysis inevitability results in activation of inflammatory processes and its efficiency is highly variable between patients. An improved method to isolate biomarkers and study pathophysiological mechanisms in peritoneal dialysis effluent (PDE) is expected to be of much benefit for the development of this treatment approach and help with patient management. Extracellular vesicles (EVs) are released as part of normal cellular processes. Their proteome is expected to reflect both type and health of their cell of origin...
2017: PloS One
https://www.readbyqxmd.com/read/28590829/aging-and-sexual-health-getting-to-the-problem
#8
Ecem Kaya, Suresh C Sikka, Philip J Kadowitz, Serap Gur
Erectile dysfunction (ED) is one of the most common disorders in male and is often associated with other age-related comorbidities. The aging process affects the structural organization and function of penile erectile components such as smooth muscle cell and vascular architecture. These modifications affect penile hemodynamics by impairing cavernosal smooth muscle cell relaxation, reducing penile elasticity, compliance and promoting fibrosis. This review aims to identify the mechanisms of ED in the penile aging process in experimental and clinical data...
June 2017: Aging Male: the Official Journal of the International Society for the Study of the Aging Male
https://www.readbyqxmd.com/read/28588484/akrinor-tm-a-cafedrine-theodrenaline-mixture-20-1-increases-force-of-contraction-of-human-atrial-myocardium-but-does-not-constrict-internal-mammary-artery-in-vitro
#9
Benjamin Kloth, Simon Pecha, Eileen Moritz, Yvonne Schneeberger, Klaus-Dieter Söhren, Edzard Schwedhelm, Hermann Reichenspurner, Thomas Eschenhagen, Rainer H Böger, Torsten Christ, Sebastian N Stehr
Background: Intraoperative hypotension is a common problem and direct or indirect sympathomimetic drugs are frequently needed to stabilize blood pressure. Akrinor(TM) consists of the direct and the indirect sympathomimetic noradrenaline and norephedrine. Both substances are covalently bound to the phosphodiesterase (PDE) inhibitor theophylline, yielding theodrenaline and cafedrine, respectively. We investigated pharmacodynamic effects of Akrinor(TM) and its constituents on contractile force and tension in human atrial trabeculae and internal A...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28588250/an-atypical-phosphodiesterase-capable-of-degrading-haloalkyl-phosphate-diesters-from-sphingobium-sp-strain-tcm1
#10
Katsumasa Abe, Naoko Mukai, Yuka Morooka, Takeshi Makino, Kenji Oshima, Shouji Takahashi, Yoshio Kera
Sphingobium sp. strain TCM1 can degrade tris(2-chloroethyl) phosphate (TCEP) to inorganic phosphate and 2-chloroethanol. A phosphotriesterase (PTE), phosphodiesterase (PDE) and phosphomonoesterase (PME) are believed to be involved in the degradation of TCEP. The PTE and PME that respectively catalyze the first and third steps of TCEP degradation in TCM1 have been identified. However, no information has been reported on a PDE catalyzing the second step. In this study, we identified, purified, and characterized a PDE capable of hydrolyzing haloalkyl phosphate diesters...
June 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28587358/a-meta-analysis-of-pde-gene-polymorphism-and-cerebral-infarction-risk
#11
Wei-Lin Wu, Xue-Wen Feng, Chen-Feng Qiu, Jing Lin, Xian-Jun Bao
Previous studies identified that phosphodiesterase 4D (PDE4D) gene polymorphism might be associated with cerebral infarction or ischemic stroke, and hemorrhagic stroke in human populations. However, as yet, no meta-analysis has revealed any detailed association. We retrospectively reviewed studies regarding the relationship of PDE4D gene polymorphism with ischemic stroke (IS) published during the period January 2003 to September 2012. According to the inclusion criteria, 9 of 105 initial studies were included in the subsequent analysis...
June 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28587325/sildenafil-suppresses-the-proliferation-and-enhances-the-apoptosis-of-hemangioma-endothelial-cells
#12
Xiaopo He, Yiran Liu, Kai Li, Aijun Yang, Rui Wang, Shaohua Liu
Treatment of infantile hemangiomas (IH) with propranolol was first reported in 2008. Regressions of lymphatic malformations combined with pulmonary hypertension was first reported in 2012 after three children received treatment with oral sildenafil, which serves as an antagonist of phosphodiesterase isoform-5 (PDE-5). A marked expression of endothelial cells in the cytoplasm of IH tissues was obtained in our previous study. Therefore, the present study hypothesized that the antagonist of PDE-5, sildenafil, may lead to the regression of hemangiomas...
June 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28583636/metabolic-profile-of-liver-damage-in-non-cirrhotic-virus-c-and-autoimmune-hepatitis-a-proton-decoupled-31-p-mrs-study
#13
Antti Hakkarainen, Lauri Puustinen, Reetta Kivisaari, Sonja Boyd, Urpo Nieminen, Perttu Arkkila, Nina Lundbom
PURPOSE: To study liver (31)P MRS, histology, transient elastography, and liver function tests in patients with virus C hepatitis (HCV) or autoimmune hepatitis (AIH) to test the hypothesis that (31)P MR metabolic profile of these diseases differ. MATERIALS AND METHODS: 25 patients with HCV (n=12) or AIH (n=13) underwent proton decoupled (31)P MRS spectroscopy performed on a 3.0T MR imager. Intensities of phosphomonoesters (PME) of phosphoethanolamine (PE) and phosphocholine (PC), phosphodiesters (PDE) of glycerophosphoethanolamine (GPE) and glycerophosphocholine (GPC), and γ, α and β resonances of adenosine triphosphate (ATP), and nicotinamide adenine dinucleotide phosphate (NADPH) were determined...
May 2017: European Journal of Radiology
https://www.readbyqxmd.com/read/28580889/phosphodiesterase-5-inhibitors-and-their-analogues-as-adulterants-of-herbal-and-food-products-analysis-of-the-malaysian-market-in-2014-2016
#14
Nur Baizura Bujang, Chin Fei Chee, Choon Han Heh, Noorsaadah Abd Rahman, Michael J C Buckle
Adulteration of herbal health supplements with phosphodiesterase-5 (PDE-5) inhibitors and their analogues is becoming a worldwide problem. The aim of this study was to investigate herbal and food products sold in the Malaysian market for the presence of these adulterants. Sixty-two products that claim to enhance men's sexual health were sampled between April 2014 and April 2016. These products included unregistered products seized by the Pharmacy Enforcement Division of the Ministry of Health (n = 39), products sent to the National Pharmaceutical Regulatory Agency for pre-registration testing (n = 9) and products investigated under the post-registration market surveillance programme (n = 14)...
June 5, 2017: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/28572694/c-arm-positioning-using-virtual-fluoroscopy-for-image-guided-surgery
#15
T De Silva, J Punnoose, A Uneri, J Goerres, M Jacobson, M D Ketcha, A Manbachi, S Vogt, G Kleinszig, A J Khanna, J-P Wolinksy, G Osgood, J H Siewerdsen
INTRODUCTION: Fluoroscopically guided procedures often involve repeated acquisitions for C-arm positioning at the cost of radiation exposure and time in the operating room. A virtual fluoroscopy system is reported with the potential of reducing dose and time spent in C-arm positioning, utilizing three key advances: robust 3D-2D registration to a preoperative CT; real-time forward projection on GPU; and a motorized mobile C-arm with encoder feedback on C-arm orientation. METHOD: Geometric calibration of the C-arm was performed offline in two rotational directions (orbit α, orbit β)...
February 11, 2017: Proceedings of SPIE
https://www.readbyqxmd.com/read/28569061/structure-based-design-of-scaffolds-targeting-pde10a-by-inpharma-nmr
#16
Luca Codutti, Manuela Grimaldi, Teresa Carlomagno
Phosphodiesterases (PDE) hydrolyze both cyclic AMP and GMP (cAMP/cGMP) and are responsible for the regulation of their levels in a multitude of cellular functions. PDE10A is expressed in the brain and is a validated target for both schizophrenia and Huntington disease. Here, we address the identification of novel chemical scaffolds that may bind PDE10A via structure-based drug design. For this task, we use INPHARMA, an NMR-based method that measures protein-mediated interligand NOEs between pairs of weakly, competitively binding ligands...
May 31, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28566262/effect-of-phosphodiesterase-5-inhibition-with-tadalafil-on-systemic-right-ventricular-size-and-function-a-multi-center-double-blind-randomized-placebo-controlled-clinical-trial-serve-trial-rational-and-design
#17
Daniel Tobler, Judith Bouchardy, Engel Reto, Dik Heg, Christian Müller, André Frenk, Harald Gabriel, Jürg Schwitter, Tobias Rutz, Ronny R Buechel, Matthias Willhelm, Lukas Trachsel, Michael Freese, Matthias Greutmann, Markus Schwerzmann
BACKGROUND: Patients with a systemic right ventricle (RV) have a compromised late outcome caused by ventricular dysfunction. Standard medical heart failure therapy has not been shown to improve RV function and survival in these patients. Phosphodiesterase (PDE)-5 inhibition increases contractility in experimental models of RV hypertrophy, but not in the normal RV. In clinical practice, the effects of PDE-5 inhibition on systemic RV function and exercise capacity in adults with a systemic RV have not been tested...
May 23, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/28558784/hesperetin-5-7-3-o-triacetate-suppresses-airway-hyperresponsiveness-in-ovalbumin-sensitized-and-challenged-mice-without-reversing-xylazine-ketamine-induced-anesthesia-in-normal-mice
#18
You-Lan Yang, Chi-Li Chen, Chi-Ming Chen, Wun-Chang Ko
BACKGROUND: We recently reported that hesperetin-5,7,3'-O-triacetate (HTA) dually inhibited phosphodiesterase (PDE)3/4 with a therapeutic ratio of 20.8. The application and development of PDE4 inhibitors for treating asthma or COPD are limited by their side effects, such as nausea, vomiting and gastric hypersecretion. PDE4 inhibitors were reported to reverse xylazine/ketamine-induced anesthesia in rats and triggered vomiting in ferrets. Thus the reversing effect of HTA on xylazine/ketamine-induced anesthesia in mice was studied to assess emetic effect of HTA...
May 30, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28554321/phosphodiesterase-4-inhibitors-in-immune-mediated-diseases-mode-of-action-clinical-applications-current-and-future-perspectives
#19
Lazaros I Sakkas, Athanasios Mavropoulos, Dimitrios P Bogdanos
Phosphodiesterase (PDE) 4 is a superfamily of enzymes that catalyze the hydrolysis of cyclic adenosine 3',5'-monophosphate (cAMP), an intracellular second messenger and regulator of a wide array of genes and proteins. Increased levels of intracellular cAMP lead to activation of genes but also to inhibition of nuclear factor-kappa B, involved in pro-inflammatory responses. By increasing cAMP levels, PDE4 inhibitors, such as apremilast, reduced production of pro-inflammatory TNFα, IFNγ, and IL-17 and increased production of anti-inflammatory IL-10 in lipopolysaccharide-stimulated peripheral blood mononuclear cells, and in patients with psoriatic arthritis (PsA)...
May 29, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28550289/heat-transfer-enhancement-in-free-convection-flow-of-cnts-maxwell-nanofluids-with-four-different-types-of-molecular-liquids
#20
Sidra Aman, Ilyas Khan, Zulkhibri Ismail, Mohd Zuki Salleh, Qasem M Al-Mdallal
This article investigates heat transfer enhancement in free convection flow of Maxwell nanofluids with carbon nanotubes (CNTs) over a vertically static plate with constant wall temperature. Two kinds of CNTs i.e. single walls carbon nanotubes (SWCNTs) and multiple walls carbon nanotubes (MWCNTs) are suspended in four different types of base liquids (Kerosene oil, Engine oil, water and ethylene glycol). Kerosene oil-based nanofluids are given a special consideration due to their higher thermal conductivities, unique properties and applications...
May 26, 2017: Scientific Reports
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