phosphodiesterase-4 (PDE4)
The effect of resveratrol on beta amyloid-induced memory impairment involves inhibition of phosphodiesterase-4 related signaling
... by phosphodiesterase (PDE) activities, the further study found that resveratrol is a PDE ...of phosphodiesterase 4 (PDE 4) inhibitors in learning and memory performance has provoked intense ...
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Can roflumilast, a phosphodiesterase-4 inhibitor, improve clinical outcomes in patients with moderate-to-severe chronic obstructive pulmonary disease? A meta-analysis
... Phosphodiesterase-4 (PDE4) is a vital enzyme in the me- tabolism of cyclic adenosine monophosphate (cAMP) and inhibition of PDE4 can inactivate immune and inflamma- tory cells via increase cAMP [9]. It is ...
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Targeting phosphodiesterase 4 as a potential therapeutic strategy for enhancing neuroplasticity following ischemic stroke
... Sensorimotor recovery following ischemic stroke is highly related with structural modification and functional reorganization of residual brain tissues. Manipulations, such as treatment with small molecules, have been ...
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Phosphodiesterase 4 inhibition in the treatment of psoriasis, psoriatic arthritis and other chronic inflammatory diseases
... inhibitors have been developed, their introduction in the clinic has been hampered by their narrow therapeutic window with side effects such as nausea and emesis occurring at sub-therapeutic levels. The latest generation ...
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Phosphodiesterase 4-targeted treatments for autoimmune diseases
... active phosphodiesterase 4 and tumor necrosis factor- α ...1, 4- cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of ...
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Roflumilast: first phosphodiesterase 4 inhibitor approved for treatment of COPD
... selective phosphodiesterase 4 inhibitor, for the “maintenance treatment of severe chronic obstructive pulmonary disease (COPD, FEV 1 postbronchodilator less than 50% predicted) associated with chronic ...
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Rolipram, a Phosphodiesterase 4 Inhibitor, Stimulates Inducible cAMP Early Repressor Expression in Osteoblasts
... 17. Miyamoto K, Waki Y, Horita T, Kasugai S, Ohya K. Reduction of bone loss by denbufylline, an inhibitor of phosphodiesterase 4. Biochem Pharmacol 1997;54:613-7. 18. Wong BR, Rho J, Arron J, Robinson E, ...
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Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors
... not interfere with apremilast, is provided by the finding that when the A 2A R was knocked down (A 2A R shRNA: 54 % Fig. 3 Apremilast inhibits lipopolysaccharide ( LPS )-induced TNF- α release via cyclic adenosine ...
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Dimerization of cAMP phosphodiesterase-4 (PDE4) in living cells requires interfaces located in both the UCR1 and catalytic unit domains
... a 4-helix bundle in dimeric PDE4 long forms (vide infra), such that hydrophobic surfaces running along the proposed helices are a major contributory feature to a dimerization ...
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The inhaled phosphodiesterase 4 inhibitor GSK256066 reduces allergen challenge responses in asthma
... The LAR is characterised by an inflammatory cell influx into the airways, comprising a variety of cell types including eosinophils, basophils and lymphocytes that are recruited by T-helper 2 (TH2) cytokines [25]. The LAR ...
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Effects of phosphodiesterase 4 inhibition on bleomycin-induced pulmonary fibrosis in mice
... For these reasons, PDE4 inhibitors were suggested for treatment of several lung diseases as new anti-inflamma- tory and anti-remodeling agents [16]. Our group has pre- viously demonstrated that PDE3/4 inhibitor ...
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The effect of the novel phosphodiesterase-4 inhibitor MEM 1414 on the allergen induced responses in mild asthma
... Reducing FeNO levels by specific iNOS inhibition does not inhibit the EAR or LAR, suggesting that nitric oxide is not mechanistically involved in the pathophysiology of allergen-induced asthma [17]. However, FeNO is a ...
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Hesperetin-7,3'-O-dimethylether selectively inhibits phosphodiesterase 4 and effectively suppresses ovalbumin-induced airway hyperresponsiveness with a high therapeutic ratio
... Hesperetin (5,7,3’-trihydroxy-4’-methoxyflavanone), one of the most-common flavonoids in Citrus, is also present in herbal medicine as glycosides. For example, hesperidin and neohesperidin are abundantly present ...
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Additive anti-inflammatory effects of corticosteroids and phosphodiesterase-4 inhibitors in COPD CD8 cells
... Fig. 3 The effect of GSK256066 with dexamethasone on cytokine release from pulmonary CD8 cells. Pulmonary CD8 cells from COPD ( n = 6) and smokers with normal lung function ( n = 4) were pre-treated with various ...
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Roflumilast, a phosphodiesterase-4 inhibitor, induces phagocytic activity in Greek COPD patients
... combination with other therapy regimens, such as LABA + ICS + LAMA and LABA + ICS. FEV 1 was not significantly improved. This is possibly due to the limited number of patients in our study or perhaps due to the short ...
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Leucine-rich repeat kinase 2 controls protein kinase A activation state through phosphodiesterase 4
... BV2 cells and mouse brains were solubilized as recently described [17]. Protein concentrations were determined using the BCA protein concentration assay as per manu- facturer’s instructions (Thermo Scientific). Fifty ...
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Apremilast for the treatment of active psoriatic arthritis: a single-centre real-life experience
... oral phosphodiesterase 4 (PDE4) inhibitor, in patients with moderate to severe plaque psoriasis: results of a phase III, randomized, controlled trial (Efficacy and Safety Trial Evaluating the Effects of ...
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Recent Developments in Atopic Dermatitis
... selective phosphodiesterase-4 (PDE4) inhibitor, in the treatment of adult and adolescent patients with mild to moderate atopic dermatitis (AD): a phase-II randomized, double-blind, placebo-controlled ...
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IN-SILICO APPROACH FOR THE IDENTIFICATION OF NEW MOLECULES FOR ALZHEIMER’S DISEASE (AD)
... Alzheimer’s disease (AD) is a malignant neurodegenerative disorder which causes the destruction of brain cells that ultimately results in memory loss and cognitive dysfunction. Deposition of b-amyloid fibril, the ...
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Expression studies of recombinant cAMP-specific phosphodiesterase type 4
... About a decade ago, Liljestrom and Garoff, 1991 developed a m amm alian expression system based on Semliki Forest Virus (SPY). This system since its development has been used to express a large number o f recombinant ...
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