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https://www.readbyqxmd.com/read/29152042/selective-inhibitors-of-phosphodiesterase-4b-pde-4b-may-provide-a-better-treatment-for-cns-metabolic-autoimmune-and-inflammatory-diseases
#1
EDITORIAL
Ahmed F Abdel-Magid
No abstract text is available yet for this article.
November 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29151951/potential-synergistic-effect-of-phosphodiesterase-inhibitors-with-chemotherapy-in-lung-cancer
#2
Kalliopi Domvri, Konstantinos Zarogoulidis, Nikolaos Zogas, Paul Zarogoulidis, Savvas Petanidis, Konstantinos Porpodis, Efrosini Kioseoglou, Wolfgang Hohenforst-Schmidt
Purpose: Lung cancer remains the leading cause of cancer-related deaths worldwide and novel therapeutic approaches targeting crucial pathways are urgently needed to improve its treatment. Differentiation-based therapeutics (Methylxanthines) and phosphodiesterase inhibitors (type 4 and 5), have been implicated in cancer treatment. Our objectives were to capture any potential anti-tumor effect of these drug combinations with chemotherapeutic agents in vitro. Methods: Theophylline as Methylxanthines, Roflumilast as phosphodiesterase type 4 (PDE4) inhibitor and Sildenafil as phosphodiesterase type 5 (PDE5) inhibitor are the drugs that we combined with the chemotherapeutic agents (Docetaxel, Cisplatin and Carboplatin) in vitro...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/29132351/therapeutic-efficacy-of-pentoxifylline-on-proteinuria-and-renal-progression-an-update
#3
REVIEW
Yung-Ming Chen, Wen-Chih Chiang, Shuei-Liong Lin, Tun-Jun Tsai
Blood pressure control with renin-angiotensin system (RAS) blockade has remained the gold standard for treating patients with proteinuric chronic kidney disease (CKD) up to date. Nevertheless, RAS blockade slows but does not halt the progression of kidney disease, thus highlighting the need to search for additional therapeutic approaches. The nonselective phosphodiesterase (PDE) inhibitor pentoxifylline (PTX) is an old drug that exhibits prominent anti-inflammatory, anti-proliferative and anti-fibrotic activities both in vitro and in vivo...
November 13, 2017: Journal of Biomedical Science
https://www.readbyqxmd.com/read/29129027/factors-affecting-the-efficacy-and-safety-of-phosphodiesterase-5-inhibitor-and-placebo-in-treatment-for-lower-urinary-tract-symptoms-meta-analysis-and-meta-regression
#4
Hwa Yeon Sun, Bora Lee, Jae Heon Kim
PURPOSE: We aimed to investigate the real benefit and safety of phosphodiesterase 5 inhibitor (PDE 5I) for benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS) by determining the affecting factors and to overcome the previous meta-analysis studies. METHODS: We conducted a systematic review of improvements in LUTS using International Prostate Symptom Score (IPSS), voiding subscore of IPSS (voiding IPSS), storage subscore of IPSS (storage IPSS), quality of life (QoL), maximal urinary flow rate (Qmax), and post-voided residual volume (PVR), and also investigated adverse events and relevant withdrawal rate...
November 11, 2017: International Urology and Nephrology
https://www.readbyqxmd.com/read/29128622/efficacy-and-tolerability-of-pharmacological-interventions-for-pulmonary-arterial-hypertension-a-network-meta-analysis
#5
Hongjing Lin, Mupeng Wang, Ying Yu, Zeyu Qin, Xin Zhong, Jiahui Ma, Fangbo Zhao, Xueli Zhang
PURPOSE: This network meta-analysis (NMA) is designed to compare the efficacy and tolerability of various therapies and combinations for pulmonary arterial hypertension (PAH). METHOD: We conducted a systematic search in databases PubMed, Embase, and Cochrane Library. Treatment efficacy and tolerability were compared by synthesizing direct and indirect evidence. The surface under the curve ranking area was utilized to rank multiple interventions. RESULT: A total of 43 randomized clinical trials were included in our NMA...
November 8, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29123207/atropine-augments-cardiac-contractility-by-inhibiting-camp-specific-phosphodiesterase-type-4
#6
Ruwan K Perera, Thomas H Fischer, Michael Wagner, Matthias Dewenter, Christiane Vettel, Nadja I Bork, Lars S Maier, Marco Conti, Juergen Wess, Ali El-Armouche, Gerd Hasenfuß, Viacheslav O Nikolaev
Atropine is a clinically relevant anticholinergic drug, which blocks inhibitory effects of the parasympathetic neurotransmitter acetylcholine on heart rate leading to tachycardia. However, many cardiac effects of atropine cannot be adequately explained solely by its antagonism at muscarinic receptors. In isolated mouse ventricular cardiomyocytes expressing a Förster resonance energy transfer (FRET)-based cAMP biosensor, we confirmed that atropine inhibited acetylcholine-induced decreases in cAMP. Unexpectedly, even in the absence of acetylcholine, after G-protein inactivation with pertussis toxin or in myocytes from M2- or M1/3-muscarinic receptor knockout mice, atropine increased cAMP levels that were pre-elevated with the β-adrenergic agonist isoproterenol...
November 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29122629/long-term-cilostazol-administration-prevents-age-related-decline-of-hippocampus-dependent-memory-in-mice
#7
Shuichi Yanai, Hideki Ito, Shogo Endo
Phosphodiesterases (PDEs) are enzymes that hydrolyze and inactivate 3', 5'-cyclic adenosine monophosphate (cAMP) and/or 3', 5'-cyclic guanosine monophosphate (cGMP). The regulation of intracellular signaling pathways mediated by cyclic nucleotides is imperative to synaptic plasticity and memory in animals. Because PDEs play an important role in this regulation, PDE inhibitors are considered as candidate compounds for treating cognitive and memory disorders. In the present study, we tested whether cilostazol, a selective PDE3 inhibitor, prevents the cognitive deterioration that occurs during the course of normal aging in mice...
November 6, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29113064/inhibition-of-cyclic-adenosine-monophosphate-specific-phosphodiesterase-by-various-food-plant-derived-phytotherapeutic-agents
#8
Teresa Röhrig, Olga Pacjuk, Silvia Hernández-Huguet, Johanna Körner, Katharina Scherer, Elke Richling
Background: Phosphodiesterases (PDEs) play a major role in the regulation of cyclic adenosine monophosphate (cAMP)- and cyclic guanosine monophosphate (cGMP)-mediated pathways. Their inhibitors exhibit anti-inflammatory, vasodilatory and antithrombotic effects. Therefore, consumption of foods with PDE-inhibiting potential may possess beneficial influence on the risk of cardiovascular diseases. Methods: Four plant extracts (Arbutus unedo, Camellia sinensis, Cynara scolymus, Zingiber officinale) with promising ingredient profiles and physiological effects were tested for their ability to inhibit cAMP-specific PDE in vitro in a radioactive assay...
November 4, 2017: Medicines (Basel, Switzerland)
https://www.readbyqxmd.com/read/29107068/targeting-tumor-cells-based-on-phosphodiesterase-3a-expression
#9
Madiha Nazir, Wojciech Senkowski, Frida Nyberg, Kristin Blom, Per-Henrik Edqvist, Malin Jarvius, Claes Andersson, Mats G Gustafsson, Peter Nygren, Rolf Larsson, Mårten Fryknäs
We and others have previously reported a correlation between high phosphodiesterase 3A (PDE3A) expression and selective sensitivity to phosphodiesterase (PDE) inhibitors. This indicates that PDE3A could serve both as a drug target and a biomarker of sensitivity to PDE3 inhibition. In this report, we explored publicly available mRNA gene expression data to identify cell lines with different PDE3A expression. Cell lines with high PDE3A expression showed marked in vitro sensitivity to PDE inhibitors zardaverine and quazinone, when compared with those having low PDE3A expression...
October 26, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/29101001/icariside-ii-a-pde5-inhibitor-from-epimedium-brevicornum-promotes-neuron-like-pheochromocytoma-pc12-cell-proliferation-via-activating-no-cgmp-pkg-pathway
#10
Jianmei Gao, Yingshu Xu, Ming Lei, Jingshan Shi, Qihai Gong
Icariside II (ICS II), a phosphodiesterase 5 inhibitor (PDE 5-I), is a major ingredient of Epimedium brevicornum, with wide spectrum of neuroprotective properties. However, little is known about the potential beneficial effect of ICS II on neuronal cell proliferation, and its possible underlying mechanism remains still unclear. We hypothesized that the beneficial effect of ICS II on neuron-like highly differentiated rat pheochromocytoma (PC12) cell proliferation is correlated with the nitric oxide (NO) signaling pathway and its upstream of PI3K/AKT pathway...
October 31, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/29098341/acute-administration-of-roflumilast-enhances-sensory-gating-in-healthy-young-humans-in-a-randomized-trial
#11
Pim R A Heckman, Marlies A Van Duinen, Arjan Blokland, Tolga Uz, Jos Prickaerts, Anke Sambeth
INTRODUCTION: Sensory gating is a process involved in early information processing which prevents overstimulation of higher cortical areas by filtering sensory information. Research has shown that the process of sensory gating is disrupted in patients suffering from clinical disorders including attention deficit hyper activity disorder, schizophrenia, and Alzheimer's disease. Phosphodiesterase (PDE) inhibitors have received an increased interest as a tool to improve cognitive performance in both animals and man, including sensory gating...
November 3, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/29094165/phosphodiesterase-inhibitors-sildenafil-and-vardenafil-reduce-zebrafish-rod-photoreceptor-outer-segment-shedding
#12
Leah J Campbell, Abbie M Jensen
Purpose: The vertebrate rod photoreceptor undergoes daily growth and shedding to renew the rod outer segment (ROS), a modified cilium that contains the phototransduction machinery. It has been demonstrated that ROS shedding is regulated by the light-dark cycle; however, we do not yet have a satisfactory understanding of the molecular mechanisms that underlie this regulation. Given that phototransduction relies on the hydrolysis of cGMP via phosphodiesterase 6 (PDE6), we examined ROS growth and shedding in zebrafish treated with cGMP-specific PDE inhibitors...
November 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/29093293/discovery-of-a-novel-series-of-pyrazolo-1-5-a-pyrimidine-based-phosphodiesterase-2a-inhibitors-structurally-different-from-n-1s-1-3-fluoro-4-trifluoromethoxy-phenyl-2-methoxyethyl-7-methoxy-2-oxo-2-3-dihydropyrido-2-3-b-pyrazine-4-1h-carboxamide-tak-915-for
#13
Satoshi Mikami, Masanori Kawasaki, Shuhei Ikeda, Nobuyuki Negoro, Shinji Nakamura, Izumi Nomura, Tomoko Ashizawa, Hironori Kokubo, Isaac Dylan Hoffman, Hua Zou, Hideyuki Oki, Noriko Uchiyama, Yuuto Hiura, Maki Miyamoto, Yuuki Itou, Masato Nakashima, Hiroki Iwashita, Takahiko Taniguchi
It has been hypothesized that selective inhibition of phosphodiesterase (PDE) 2A could potentially be a novel approach to treat cognitive impairment in neuropsychiatric and neurodegenerative disorders through augmentation of cyclic nucleotide signaling pathways in brain regions associated with learning and memory. Following our earlier work, this article describes a drug design strategy for a new series of lead compounds structurally distinct from our clinical candidate 2 (TAK-915), and subsequent medicinal chemistry efforts to optimize potency, selectivity over other PDE families, and other preclinical properties including in vitro phototoxicity and in vivo rat plasma clearance...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29089445/novel-imaging-of-the-prostate-reveals-spontaneous-gland-contraction-and-excretory-duct-quiescence-together-with-different-drug-effects
#14
Robert Kügler, Andrea Mietens, Mathias Seidensticker, Sabine Tasch, Florian M Wagenlehner, Andre Kaschtanow, Yudy Tjahjono, Claudia U Tomczyk, Daniela Beyer, Gail P Risbridger, Betty Exintaris, Stuart J Ellem, Ralf Middendorff
Prostate carcinoma and benign prostate hyperplasia (BPH) with associated lower urinary tract symptoms (LUTS) are among the most prevalent and clinically relevant diseases in men. BPH is characterized by an enlargement of prostate tissue associated with increased tone of smooth muscle cells (SMCs) which surround the single glands composing the prostate. Secretions of the glands leave the prostate through local excretory ducts during the emission phase of ejaculation. Pharmacological treatment of BPH suggests different local drug targets based on reduction of prostate smooth muscle tone as the main effect and disturbed ejaculation as a common side effect...
October 31, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29067241/effect-of-phosphodiesterase-5-inhibitors-on-glycemic-control-in-person-with-type-2-diabetes-mellitus-a-systematic-review-and-meta-analysis
#15
Nalinee Poolsup, Naeti Suksomboon, Nandar Aung
Chronic use of phosphodiesterase-5 inhibitors (PDE-5i) has been shown to improve insulin action on muscle glucose uptake by the prolongation of nitric oxide (NO)/cyclic guanosine monophosphate (cGMP)/protein kinase (PKG) signalling. AIMS: As the effects of PDE-5i on glycemic control in person with type 2 diabetes mellitus (T2DM) have not been systematically explored, we conducted a meta-analysis of available randomized controlled trials (RCTs). METHODS: A literature search was performed through electronic databases including MEDLINE (Pubmed), The Cochrane Library, SCOPUS, Web of Science, CINAHL, www...
December 2016: Journal of Clinical & Translational Endocrinology
https://www.readbyqxmd.com/read/29042668/signalling-mechanisms-in-paf-induced-intestinal-failure
#16
Ingmar Lautenschläger, Yuk Lung Wong, Jürgen Sarau, Torsten Goldmann, Karina Zitta, Martin Albrecht, Inéz Frerichs, Norbert Weiler, Stefan Uhlig
Capillary leakage syndrome, vasomotor disturbances and gut atony are common clinical problems in intensive care medicine. Various inflammatory mediators and signalling pathways are involved in these pathophysiological alterations among them platelet-activating factor (PAF). The related signalling mechanisms of the PAF-induced dysfunctions are only poorly understood. Here we used the model of the isolated perfused rat small intestine to analyse the role of calcium (using calcium deprivation, IP-receptor blockade (2-APB)), cAMP (PDE-inhibition plus AC activator), myosin light chain kinase (inhibitor ML-7) and Rho-kinase (inhibitor Y27632) in the following PAF-induced malfunctions: vasoconstriction, capillary and mucosal leakage, oedema formation, malabsorption and atony...
October 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29029361/the-mechanism-of-attenuation-of-epithelial-mesenchymal-transition-by-a-phosphodiesterase-5-inhibitor-via-renal-klotho-expression
#17
Seung Tae Han, Jae Seok Kim, Jun Young Lee, Min Keun Kim, Jin Sae Yoo, Byoung Geun Han, Seung Ok Choi, Jae Won Yang
OBJECTIVES: Phosphodiesterase-5 (PDE-5) inhibitors induces vasodilation in several organs by blocking cyclic GMP (guanosine monophosphate) degradation. However, the existence of alternative mechanism of action in case of an impaired nitric oxide (NO) system remains controversial. Previous studies suggested that decreased NO bioavailability may result in the down-regulation of klotho expression, but the relationship between klotho and NO remains obscure. Therefore, we investigated whether a PDE-5 inhibitor could preserve epithelial mesenchymal transition (EMT) and relationship exists between the NO and renal klotho expression...
October 13, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/29016851/mutations-causing-acrodysostosis-2-facilitate-activation-of-phosphodiesterase-4d3
#18
Claire Briet, Arrate Pereda, Catherine Le Stunff, Emmanuelle Motte, Juan de Dios Garcia-Diaz, Guiomar Perez de Nanclares, Nicolas Dumaz, Caroline Silve
Type 2 acrodysostosis (ACRDYS2), a rare developmental skeletal dysplasia characterized by short stature, severe brachydactyly and facial dysostosis, is caused by mutations in the phosphodiesterase (PDE) 4D (PDE4D) gene. Several arguments suggest that the mutations should result in inappropriately increased PDE4D activity, however, no direct evidence supporting this hypothesis has been presented, and the functional consequences of the mutations remain unclear. We evaluated the impact of four different PDE4D mutations causing ACRDYS2 located in different functional domains on the activity of PDE4D3 expressed in Chinese hamster ovary cells...
October 15, 2017: Human Molecular Genetics
https://www.readbyqxmd.com/read/28959341/expression-of-recombinant-phosphodiesterases-3a-and-3b-using-baculovirus-expression-system
#19
Yongmin Yan, Wenqian Jiang, Jingwen Liu, Wenrong Xu, Hui Qian
BACKGROUND: Phosphodiesterase 3A (PDE3A) and phosphodiesterase 3B (PDE3B) play a critical role in the regulation of intracellular level of adenosine 3´,5´-cyclic monophosphate (cyclic AMP, cAMP) and guanosine 3´,5´-cyclic monophosphate (cyclic GMP, cGMP). Subsequently PDE3 inhibitors have shown to relax vascular and inhibit platelet aggregation in cardiovascular disease. OBJECTIVES: In this study, our aim was to establish a method of expression for the recombinant human PDE3A and PDE3B proteins in insect cells using baculovirus expression system in order to investigate the activity of the expressed PDE3A and PDE3B proteins...
December 2016: Iranian journal of biotechnology
https://www.readbyqxmd.com/read/28957634/the-discovery-of-a-novel-phosphodiesterase-pde-4b-preferring-radioligand-for-positron-emission-tomography-pet-imaging
#20
Lei Zhang, Laigao Chen, Elizabeth M Beck, Thomas A Chappie, Richard V Coelho, Shawn D Doran, Kuo-Hsien Fan, Christopher J Helal, John M Humphrey, Zoe Hughes, Kyle Kuszpit, Erik A Lachapelle, John T Lazzaro, Chewah Lee, Robert J Mather, Nandini C Patel, Marc B Skaddan, Simone Sciabola, Patrick R Verhoest, Joseph M Young, Kenneth Zasadny, Anabella Villalobos
As part of our effort in identifying phosphodiesterase (PDE) 4B-preferring inhibitors for the treatment of central nervous system (CNS) disorders, we sought to identify a positron emission tomography (PET) ligand to enable target occupancy measurement in vivo. Through a systematic and cost-effective PET discovery process, involving expression level (Bmax) and biodistribution determination, a PET-specific structure-activity relationship (SAR) effort, and specific binding assessment using a LC-MS/MS "cold tracer" method, we have identified 8 (PF-06445974) as a promising PET lead...
October 9, 2017: Journal of Medicinal Chemistry
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