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Phosphodiesterase 4

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https://www.readbyqxmd.com/read/29155261/the-phosphodiesterase-4-inhibitor-fcpr16-attenuates-ischemia-reperfusion-injury-in-rats-subjected-to-middle-cerebral-artery-occlusion-and-reperfusion
#1
Jiajia Chen, Hui Yu, Jiahong Zhong, Hongfang Feng, Haitao Wang, Yufang Cheng, Zhengqiang Zou, Chang Huang, Zhongzhen Zhou, Wenhua Zheng, Jiangping Xu
Current phosphodiesterase-4 (PDE4) inhibitors exert beneficial effects in central nervous system diseases via anti-inflammatory and anti-apoptotic properties, but many of them are plagued by side effects like nausea and emesis. FCPR16, a novel PDE4 inhibitor synthesized in our lab, has potential anti-inflammatory property. In the present study, we aimed to investigate the effects of FCPR16 in a rat model of ischemic stroke and evaluate its emetogenic potential. Our results showed that FCPR16 treatment improved neurological function, reduced cerebral infarct volume, and attenuated brain histological changes in rats subjected to middle cerebral artery occlusion and reperfusion (MCAO/R)...
November 16, 2017: Brain Research Bulletin
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/29141319/-homozygous-ectonucleotide-pyrophosphatase-phosphodiesterase-1-variants-in-a-girl-with-hypophosphatemic-rickets-and-literature-review
#3
Z Q Liu, X B Chen, F Y Song, K Gao, M F Qiu, Y Qian, M Du
Objective: To investigate the clinical features and genetic characteristics of patients with ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) gene variants. Method: The clinical data of a patient with ENPP1 homozygous variants from Capital Institute of Pediatrics was collected, the related literature was searched from China National Knowledge Infrastructure, Wanfang Data Knowledge Service Platform, National Center from Biotechnology Information and PubMed by using search term "ENPP1" , "hypophosphatemic rickets" ...
November 2, 2017: Zhonghua Er Ke za Zhi. Chinese Journal of Pediatrics
https://www.readbyqxmd.com/read/29138698/soluble-epoxide-hydrolase-inhibitor-and-14-15-epoxyeicosatrienoic-acid-facilitated-long-term-potentiation-through-camp-and-camkii-in-the-hippocampus
#4
Han-Fang Wu, Yi-Ju Chen, Su-Zhen Wu, Chi-Wei Lee, I-Tuan Chen, Yi-Chao Lee, Chi-Chen Huang, Chung-Hsi Hsing, Chih-Wei Tang, Hui-Ching Lin
Epoxyeicosatrienoic acids (EETs) are derived from arachidonic acid and metabolized by soluble epoxide hydrolase (sEH). The role of EETs in synaptic function in the central nervous system is still largely unknown. We found that pharmacological inhibition of sEH to stabilize endogenous EETs and exogenous 14,15-EET significantly increased the field excitatory postsynaptic potential (fEPSP) response in the CA1 area of the hippocampus, while additionally enhancing high-frequency stimulation- (HFS-) induced long-term potentiation (LTP) and forskolin- (FSK-) induced LTP...
2017: Neural Plasticity
https://www.readbyqxmd.com/read/29130985/heptamethoxyflavone-reduces-phosphodiesterase-activity-and-t-cell-growth-in-vitro
#5
Yui Hamada, Mitsunari Nakajima, Kazuna Tsuzuki, Yoshiaki Amakura, Morio Yoshimura, Satoshi Okuyama, Yoshiko Furukawa
In a previous study, we reported that interleukin-4 production was reduced in spleen cells of mice administered 3,5,6,7,8,3',4'-heptamethoxyflavone (HMF), which is a polymethoxyflavone found at high concentrations in the peel of various citrus fruits. In this study, we investigated the function of HMF on the growth of T cells cultured from the spleens of mice. HMF decreased the reduction of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) by anti-CD3/CD28 antibody-stimulated mouse spleen cells...
November 8, 2017: International Archives of Allergy and Immunology
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/29122494/penile-rehabilitation-therapy-following-radical-prostatectomy-a-meta-analysis
#7
REVIEW
Chunhui Liu, David S Lopez, Ming Chen, Run Wang
BACKGROUND: Penile rehabilitation, defined as the use of any drug or device at or after radical prostatectomy to maximize erectile function recovery, is commonly used for post-prostatectomy erectile dysfunction; however, conflicting results based on each study make it difficult to give a recommendation for clinical practice. AIM: To clarify the effect of oral phosphodiesterase type 5 inhibitors (PDE5is), vacuum erection devices, intracorporeal injection therapy, and the combination of these treatments on penile rehabilitation...
November 6, 2017: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/29119630/mycobacterium-tuberculosis-rv3651-is-a-triple-sensor-domain-protein
#8
Jan Abendroth, Andrew Frando, Isabelle Q Phan, Bart L Staker, Peter J Myler, Thomas E Edwards, Christoph Grundner
The genome of the human pathogen Mycobacterium tuberculosis (Mtb) encodes ∼4,400 proteins, but one third of them have unknown functions. We solved the crystal structure of Rv3651, a hypothetical protein with no discernible similarity to proteins with known function. Rv3651 has a three-domain architecture that combines one cGMP-specific phosphodiesterases, adenylyl cyclases and FhlA (GAF) domain and two Per-ARNT-Sim (PAS) domains. GAF and PAS domains are typically sensor domains that are linked to signaling effector molecules...
November 9, 2017: Protein Science: a Publication of the Protein Society
https://www.readbyqxmd.com/read/29113762/the-identification-of-a-novel-lead-class-for-phosphodiesterase-2-inhibition-by-fragment-based-drug-design
#9
Ashley B Forster, Pravien Abeywickrema, Jaime Bunda, Christopher D Cox, Tamara D Cabalu, Melissa Egbertson, John Fay, Krista Getty, Dawn Hall, Maria Kornienko, Jun Lu, Gopal Parthasarathy, John Reid, Sujata Sharma, William D Shipe, Sean M Smith, Stephen Soisson, Shawn J Stachel, Hua-Poo Su, Deping Wang, Richard Berger
We have identified a novel PDE2 inhibitor series using fragment-based screening. Pyrazolopyrimidine fragment 1, while possessing weak potency (Ki = 22.4 μM), exhibited good binding efficiencies (LBE = 0.49, LLE = 4.48) to serve as a start for structure-based drug design. With the assistance of molecular modeling and X-ray crystallography, this fragment was developed into a series of potent PDE2 inhibitors with good physicochemical properties. Compound 16, a PDE2 selective inhibitor, was identified that exhibited favorable rat pharmacokinetic properties...
October 23, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29113064/inhibition-of-cyclic-adenosine-monophosphate-specific-phosphodiesterase-by-various-food-plant-derived-phytotherapeutic-agents
#10
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/29112590/effect-of-andrographolide-on-gene-expression-profile-and-intracellular-calcium-in-primary-rat-myocardium-microvascular-endothelial-cells
#11
Bo Feng, Qian Zhang, Xin Wang, Xiangwan Sun, Xiang Mu, Hong Dong
Andrographolide (ANDRO) is a diterpene lactone compound with extensive biological effects, such as antibacterial, antitumor and treatment of cardiovascular diseases. Until now, studies on the pharmacological functions of ANDRO are still in progress. However, little is known about the gene expression profile and calcium response of endothelial cells to ANDRO. In this study, we used a microarray technology to investigate the gene expression responses in primary rat myocardium microvascular endothelial cells (RMMECs) treated with 10μg/mL ANDRO...
October 31, 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/29107895/evaluating-the-protective-effect-of-etazolate-on-memory-impairment-anxiety-and-depression-like-behaviors-induced-by-post-traumatic-stress-disorder
#12
Karem H Alzoubi, Zeinab Y Al Subeh, Omar F Khabour
Post-traumatic stress disorder (PTSD) is a neuropsychiatric disorder that develops after an individual experiences severe life-threatening traumatic stress. Etazolate is a selective phosphodiesterase-4 inhibitor that is specific for cAMP. Etazolate showed anxiolytic and antidepressant activity, and could be useful in managing PTSD co-morbidities. The current study was done to evaluate the role of etazolate in preventing PTSD induced memory impairment, anxiety and depression-like symptoms. PTSD was induced in rats using single prolonged stress model...
November 3, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/29098911/targeted-treatments-for-hidradenitis-suppurativa-a-review-of-the-current-literature-and-ongoing-clinical-trials
#13
Melody Maarouf, Ashley K Clark, Dylan E Lee, Vivian Y Shi
PURPOSE: Targeted, immune-modulating drugs are at the forefront of therapy for HS, and a comprehensive clinical trial registry is needed to facilitate data pooling and clinical efficacy comparison. MATERIALS AND METHODS: A systematic review of the ClinicalTrials.gov database was searched for planned, in-progress, completed, or terminated trials investigating the effect of targeted biologic therapies for hidradenitis suppurativa (HS). When results of RCTs were not available, case reports or series were included...
November 10, 2017: Journal of Dermatological Treatment
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
#14
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/29092891/sildenafil-is-associated-with-reduced-device-thrombosis-and-ischemic-stroke-despite-low-level-hemolysis-on-heart-mate-ii-support
#15
Omar Saeed, Sabarivinoth Rangasamy, Ibrahim Selevany, Shivank Madan, Jeremy Fertel, Ruth Eisenberg, Mohammad Aljoudi, Snehal R Patel, Julia Shin, Daniel B Sims, Morayma Reyes Gil, Daniel J Goldstein, Marvin J Slepian, Henny H Billett, Ulrich P Jorde
BACKGROUND: Persistent low-level hemolysis (LLH) during continuous-flow mechanical circulatory support is associated with subsequent thrombosis. Free hemoglobin from ongoing hemolysis scavenges nitric oxide (NO) to create an NO deficiency which can augment platelet function leading to a prothrombotic state. The phosphodiesterase-5 inhibitor, sildenafil, potentiates NO signaling to inhibit platelet function. Accordingly, we investigated the association of sildenafil administration and thrombotic events in patients with LLH during Heart Mate II support...
November 2017: Circulation. Heart Failure
https://www.readbyqxmd.com/read/29076116/crisaborole-ointment-2-a-review-in-mild-to-moderate-atopic-dermatitis
#16
Sheridan M Hoy
Crisaborole ointment 2% (Eucrisa™) is a novel, anti-inflammatory inhibitor of phosphodiesterase 4 (PDE4) that is available in the USA for the topical treatment of mild to moderate atopic dermatitis in patients aged ≥ 2 years. In two short-term (28 days), identically designed, multicentre, phase III studies in this patient population, topical therapy with crisaborole ointment 2% reduced disease severity and pruritus severity compared with vehicle, with the effect established early and sustained over the course of treatment...
October 26, 2017: American Journal of Clinical Dermatology
https://www.readbyqxmd.com/read/29068290/otezla-warts-and-all-racks-up-sales-and-eyes-blockbuster-status
#17
Thomas Reinke
Otezla-the generic name is apremilast-also exploited a new mechanism of action as the first inhibitor of phosphodiesterase 4 (PDE4) that results in increased expression of both anti-inflammatory proteins and reduced expression of their pro-inflammatory counterparts.
October 2017: Managed Care
https://www.readbyqxmd.com/read/29068253/topical-e6005-rvt-501-a-novel-phosphodiesterase-4-inhibitor-for-the-treatment-of-atopic-dermatitis
#18
Masutaka Furue, Takafumi Kadono, Gaku Tsuji, Takeshi Nakahara
Local adverse effects of steroid use and the burning sensation of calcineurin inhibitors impair patients' adherence to treatment and decrease the treatment response in atopic dermatitis (AD). Steroid phobia appears to be a psychological problem in patients with AD. Topical non-steroidal remedies are in demand. Areas covered: This manuscript reviews the current literature on preclinical and clinical studies regarding topical E6005/RVT-501, a novel phosphodiesterase 4 inhibitor. We also discuss the mechanistic background of E6005/RVT-501 in the treatment of AD...
October 31, 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/29051185/cgmp-elevating-compounds-and-ischemic-conditioning-provide-cardioprotection-against-ischemia-and-reperfusion-injury-via-cardiomyocyte-specific-bk-channels
#19
Sandra Frankenreiter, Piotr Bednarczyk, Angelina Kniess, Nadja Bork, Julia Straubinger, Piotr Koprowski, Antoni Wrzosek, Eva Mohr, Angela Logan, Michael P Murphy, Meinrad Gawaz, Thomas Krieg, Adam Szewczyk, Viacheslav O Nikolaev, Peter Ruth, Robert Lukowski
Background -The nitric oxide-sensitive guanylyl cyclase (NO-GC)/cyclic guanosine-3',5'-monophosphate (cGMP)/cGMP-dependent protein kinase type I (cGKI)-signaling pathway can afford protection against the ischemia and reperfusion (I/R) injury that occurs during myocardial infarction (MI). Reportedly, voltage and Ca(2+)-activated K(+) channels of the BK-type are stimulated by cGMP/cGKI and recent ex-vivo studies implicated that increased BK activity favors the survival of the myocardium at I/R. It remains unclear, however, whether the molecular events downstream of cGMP involve BK channels present in cardiomyocytes (CMs) or in other cardiac cell types...
October 19, 2017: Circulation
https://www.readbyqxmd.com/read/29033813/recurrence-of-melanoma-after-starting-apremilast-for-psoriasis
#20
Thomas G Salopek
This is a report on a 32-year-old man with a history of two previous melanomas with concurrent plaque-type psoriasis. His history dates to 2009, when he was diagnosed with his first melanoma on the right occiput, Clark's level IV, tumor thickness 1.53 mm, nonulcerated, mitotic index 1/mm(2). He subsequently developed nodal recurrence after an initial negative sentinel lymph node biopsy and was treated with complete lymph node dissection. In 2012, he was diagnosed with a second primary melanoma on the right upper chest, Clark's level IV, tumor thickness 0...
May 2017: Case Reports in Dermatology
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