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Phosphodiesterase

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https://www.readbyqxmd.com/read/28642047/erectile-dysfunction-in-young-men-a-review-of-the-prevalence-and-risk-factors
#1
REVIEW
Hoang Minh Tue Nguyen, Andrew T Gabrielson, Wayne J G Hellstrom
INTRODUCTION: Erectile dysfunction (ED) is an important health concern that can significantly affect a man's psychosocial well-being. ED has traditionally been considered a disease of old age; however, contemporary evidence suggests a growing incidence of ED in men younger than 40 years. The process of achieving an erection is multifaceted; there are many potential mechanisms that can be disrupted. It is critical to identify the specific causes of ED before proceeding with potentially costly and invasive therapeutic options...
June 19, 2017: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/28640077/improvement-of-peripheral-artery-disease-with-sildenafil-and-bosentan-combined-therapy-in-a-patient-with-limited-cutaneous-systemic-sclerosis-a-case-report
#2
Loukman Omarjee, Cedric Fontaine, Guillaume Mahe, Vincent Jaquinandi
RATIONALE: Sildenafil, a phosphodiesterase-5-inhibitor and Bosentan, an endothelin-1-receptor antagonist combined therapy could have beneficial effect in systemic sclerosis (SSc) patients with peripheral artery disease. PATIENT CONCERNS: We report a case of a 48-year-old Black woman, who developed severe left limb claudication and walking limitation following a left femoropopliteal bypass occlusion in 2014. She was a heavy smoker and had a history of right middle cerebral artery ischemic stroke and bilateral Raynaud phenomenon...
June 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28638635/crystal-structure-of-an-apremilast-ethanol-hemisolvate-hemihydrate-solvatomorph
#3
Yun-Deng Wu, Xiao-Hong Liu, Jian Xu, Si-Han Zhang, Kun Shen, Ling Sun, Yong-Mei He, Yan Ma, Ai-Hua Zhang
The title compound, C22H24N2O7S·0.5C2H5OH·0.5H2O {systematic name: (S)-4-acetamido-2-[1-(3-eth-oxy-4-meth-oxy-phen-yl)-2-(methyl-sulfon-yl)eth-yl]iso-indo-line-1,3-dione ethanol hemisolvate hemihydrate}, is a novel solvatomorph of apremilast (AP), which is an inhibitor of phosphodiesterase 4 (PDE4) and is indicated for the treatment of adult patients with active psoriatic arthritis. The asymmetric unit contains one mol-ecule of AP and disordered mol-ecules of ethanol and water, both with half occupancy. The dihedral angle between the planes of the phenyl ring and the iso-indole ring is 67...
June 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28637505/human-lung-and-monocyte-derived-macrophages-differ-with-regard-to-the-effects-of-%C3%AE-2-adrenoceptor-agonists-on-cytokine-release
#4
Tatiana Victoni, Hélène Salvator, Charlotte Abrial, Marion Brollo, Luis Cristovão Sobrino Porto, Vincent Lagente, Emmanuel Naline, Stanislas Grassin-Delyle, Philippe Devillier
BACKGROUND: β2-adrenoceptor agonists have been shown to reduce the lipopolysaccharide (LPS)-induced cytokine release by human monocyte-derived macrophages (MDMs). We compare the expression of β2-adrenoceptors and the inhibitory effect of formoterol and salmeterol on the LPS-induced release of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6 and a range of chemokines (CCL2, 3, 4, and IL-8) by human lung macrophages (LMs) and MDMs. METHODS: LMs were isolated from patients undergoing resection and MDMs were obtained from blood monocytes in the presence of GM-CSF...
June 21, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28636912/channeling-of-camp-in-pde-pka-complexes-promotes-signal-adaptation
#5
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
#6
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/28628863/simultaneous-quantification-of-endothelin-receptor-antagonists-and-phosphodiesterase-5-inhibitors-currently-used-in-pulmonary-arterial-hypertension
#7
Yeliz Enderle, Lukas Witt, Heinrike Wilkens, Ekkehard Grünig, Walter E Haefeli, Jürgen Burhenne
Combination treatment with endothelin receptor antagonists (ERA) and phosphodiesterase 5 inhibitors (PDE5I) improved efficacy of pulmonary arterial hypertension (PAH) therapy. However, drug-drug interactions, variable exposure, non-adherence can influence plasma levels. For these reasons, drug quantification may be advantageous particularly in patients with poor treatment responses. We developed, validated, and applied an assay for the simultaneous quantification of ambrisentan, bosentan, macitentan, sildenafil, and tadalafil as well as their main (and partly active) metabolites in human plasma...
June 10, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28626017/amyloid-beta-peptide-is-needed-for-cgmp-induced-long-term-potentiation-and-memory
#8
Agostino Palmeri, Roberta Ricciarelli, Walter Gulisano, Daniela Rivera, Claudia Rebosio, Elisa Calcagno, Maria Rosaria Tropea, Silvia Conti, Utpal Das, Subhojit Roy, Maria A Pronzato, Ottavio Arancio, Ernesto Fedele, Daniela Puzzo
High levels of amyloid-beta peptide (Aβ) have been related to Alzheimer's disease pathogenesis. However, in the healthy brain, low physiologically relevant concentrations of Aβ are necessary for long-term potentiation (LTP) and memory. Because cGMP plays a key role in these processes, here we investigated whether the cyclic nucleotide cGMP influences Aβ levels and function during LTP and memory. We demonstrate that the increase of cGMP levels by the phosphodiesterase-5 inhibitors (PDE5-Is) sildenafil and vardenafil induces a parallel release of Aβ due to a change in the approximation of amyloid precursor protein (APP) and the β-site APP cleaving enzyme 1 (BACE1)...
June 16, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28623462/in-silico-investigations-of-chemical-constituents-of-clerodendrum-colebrookianum-in-the-anti-hypertensive-drug-targets-rock-ace-and-pde5
#9
Hemant Arya, Safiulla Basha Syed, Sorokhaibam Sureshkumar Singh, Dinakar R Ampasala, Mohane Selvaraj Coumar
Understanding the molecular mode of action of natural product is a key step for developing drugs from them. In this regard, this study is aimed to understand the molecular-level interactions of chemical constituents of Clerodendrum colebrookianum Walp., with anti-hypertensive drug targets using computational approaches. The plant has ethno-medicinal importance for the treatment of hypertension and reported to show activity against anti-hypertensive drug targets-Rho-associated coiled-coil protein kinase (ROCK), angiotensin-converting enzyme, and phosphodiesterase 5 (PDE5)...
June 16, 2017: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/28620954/propentofylline-phosphodiesterase-and-adenosine-reuptake-inhibitor-modulates-lymphocyte-subsets-and-lymphocyte-activity-after-in-vivo-administration-in-non-immunized-and-srbc-immunized-mice
#10
Marianna Szczypka, Magdalena Lis, Agnieszka Suszko-Pawłowska, Aleksandra Pawlak, Angelika Sysak, Bożena Obmińska-Mrukowicz
OBJECTIVES: The aim of the study was to investigate immunomodulatory effect of in-vivo administered propentofylline on the subsets and activity of murine lymphocytes. METHODS: Propentofylline (3 mg/kg) was administered orally to 8-week-old Balb/c mice, once or six times at 12-h intervals. The lymphocyte subsets, regulatory T cells, IL-5 and TNF levels were determined 12 h and 24 h after a single dose or after the sixth dose of the drug in non-immunized mice. Humoral immune response in sheep red blood cells (SRBC)-immunized mice was determined 4, 7 and 14 days after immunization...
June 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28620011/dietary-restriction-but-not-angiotensin-ii-type-1-receptor-blockade-improves-dna-damage-related-vasodilator-dysfunction%C3%A2-in-rapidly-aging-ercc1-%C3%AE-mice
#11
Haiyan Wu, Bibi S van Thiel, Paula Katherine Bautista-Nino, Erwin Reiling, Matej Durik, Frank P J Leijten, Yanto Ridwan, Renata M C Brandt, Harry van Steeg, Martijn E T Dollé, Wilbert P Vermeij, Jan H J Hoeijmakers, Jeroen Essers, Ingrid van der Pluijm, A H Jan Danser, Anton J M Roks
DNA damage is an important contributor to endothelial dysfunction and age-related vascular disease. Recently, we demonstrated in a DNA repair-deficient, prematurely aging mouse model ( Ercc1(∆/-) mice) that dietary restriction (DR) strongly increases life- and health span, including ameliorating endothelial dysfunction, by preserving genomic integrity. In this mouse mutant displaying prominent accelerated, age-dependent endothelial dysfunction we investigated the signaling pathways involved in improved endothelium-mediated vasodilation by DR, and explore the potential role of the renin-angiotensin system ...
June 15, 2017: Clinical Science (1979-)
https://www.readbyqxmd.com/read/28618988/synthesis-docking-and-anti-inflammatory-activity-of-triazole-amine-derivatives-as-potential-phosphodiesterase-4-inhibitors
#12
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/28617319/pde4-inhibition-and-inflammatory-bowel-disease-a-novel-therapeutic-avenue
#13
REVIEW
Marco Spadaccini, Silvia D'Alessio, Laurent Peyrin-Biroulet, Silvio Danese
BACKGROUND: In the last few decades, a better knowledge of the inflammatory pathways involved in the pathogenesis of Inflammatory Bowel Disease (IBD) has promoted biological therapy as an important tool to treat IBD patients. However, in spite of a wider spectrum of biological drugs, a significant proportion of patients is unaffected by or lose their response to these compounds, along with increased risks of infections and malignancies. For these reasons there is an urgent need to look for new pharmacological targets...
June 15, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28615646/hydrogen-sulfide-stimulates-cftr-in-xenopus-oocytes-by-activation-of-the-camp-pka-signalling-axis
#14
Alexander Perniss, Kathrin Preiss, Marcel Nier, Mike Althaus
Hydrogen sulfide (H2S) has been recognized as a signalling molecule which affects the activity of ion channels and transporters in epithelial cells. The cystic fibrosis transmembrane conductance regulator (CFTR) is an epithelial anion channel and a key regulator of electrolyte and fluid homeostasis. In this study, we investigated the regulation of CFTR by H2S. Human CFTR was heterologously expressed in Xenopus oocytes and its activity was electrophysiologically measured by microelectrode recordings. The H2S-forming sulphur salt Na2S as well as the slow-releasing H2S-liberating compound GYY4137 increased transmembrane currents of CFTR-expressing oocytes...
June 14, 2017: Scientific Reports
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
#15
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/28611079/elevated-camp-improves-signal-to-noise-ratio-in-amphibian-rod-photoreceptors
#16
Luba A Astakhova, Darya A Nikolaeva, Tamara V Fedotkina, Victor I Govardovskii, Michael L Firsov
The absolute sensitivity of vertebrate retinas is set by a background noise, called dark noise, which originates from several different cell types and is generated by different molecular mechanisms. The major share of dark noise is produced by photoreceptors and consists of two components, discrete and continuous. Discrete noise is generated by spontaneous thermal activations of visual pigment. These events are undistinguishable from real single-photon responses (SPRs) and might be considered an equivalent of the signal...
June 13, 2017: Journal of General Physiology
https://www.readbyqxmd.com/read/28607126/mechanisms-and-treatment-of-halogen-inhalation-induced-pulmonary-and-systemic-injuries-in-pregnant-mice
#17
James A Lambert, Matthew A Carlisle, Adam Lam, Saurabh Aggarwal, Stephen Doran, Changchun Ren, Wayne E Bradley, Louis Dell'Italia, Namasivayam Ambalavanan, David A Ford, Rakesh P Patel, Tamas Jilling, Sadis Matalon
Inhalation of oxidant gases has been implicated in adverse outcomes in pregnancy, but animal models to address mechanisms and studies to identify potential pregnancy-specific therapies are lacking. Herein, we show that inhalation of bromine at 600 parts per million for 30 minutes by pregnant mice on the 15th day of embryonic development results in significantly lower survival after 96 hours than an identical level of exposure in nonpregnant mice. On the 19th embryonic day, bromine-exposed pregnant mice have increased systemic blood pressure, abnormal placental development, severe fetal growth restriction, systemic inflammation, increased levels of circulating antiangiogenic short fms-like tyrosine kinase-1, and evidence of pulmonary and cardiac injury...
June 12, 2017: Hypertension
https://www.readbyqxmd.com/read/28606099/pulmonary-hemodynamics-and-effects-of-phosphodiesterase-type-5-inhibition-in-heart-failure-a-meta-analysis-of-randomized-trials
#18
In-Chang Hwang, Yong-Jin Kim, Jun-Bean Park, Yeonyee E Yoon, Seung-Pyo Lee, Hyung-Kwan Kim, Goo-Yeong Cho, Dae-Won Sohn
BACKGROUND: Previous studies suggested that phosphodiesterase 5 inhibitors (PDE5i) have a beneficial effect in patients with heart failure (HF), although the results were inconsistent. We performed a meta-analysis to evaluate the effect of PDE5i in HF patients, and investigated the relationship between PDE5i effects and pulmonary hemodynamics. METHOD: We searched PubMed, EMBASE and the Cochrane Library for randomized controlled trials (RCTs) that compared PDE5i with placebo in HF with reduced ejection fraction (HFrEF) or HF with preserved EF (HFpEF)...
June 12, 2017: BMC Cardiovascular Disorders
https://www.readbyqxmd.com/read/28605937/are-phosphodiesterase-5-inhibitors-a-sort-of-panacea-for-several-urological-diseases
#19
Guido Giusti, Silvia Proietti
no abstract.
June 12, 2017: Journal of Endourology
https://www.readbyqxmd.com/read/28605578/roflupram-a-phosphodiesterase-4-inhibitior-suppresses-inflammasome-activation-through-autophagy-in-microglial-cells
#20
Tingting You, Yu-Fang Cheng, Jiahong Zhong, Bingtian Bi, Bingqing Zeng, Wenhua Zheng, Hai-Tao Wang, Jiang-Ping Xu
Inhibition of phosphodiesterase 4 (PDE4) suppressed the inflammatory responses in the brain. However, the underlying mechanisms are poorly understood. Roflupram (ROF) is a novel PDE4 inhibitor. In the present study, we found that ROF enhanced the level of microtubule-associated protein 1 light chain 3 II (LC3-II) and decreased p62 in microglial BV-2 cells. Enhanced fluorescent signals were observed in BV-2 cells treated with ROF by Lysotracker red and acridine orange staining. In addition, immunofluorescence indicated a significant increase in punctate LC3...
June 12, 2017: ACS Chemical Neuroscience
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