Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 16 of 16 for “"PDE4"”.
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Biochemical investigation of phosphodiesterase type IV post-translational modification, cellular localisation and interaction with associated binding proteins
… In this study post-translational-modification of PDE4 isoforms is investigated. SUMOylation is a relatively newly identified post-translational modification that is known to regulate the structure and function of its substrates. PDE4 isoforms of the PDE4A and 4D subfamilies are SUMOylated by an E3 …
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The Effect of Phosphodiesterase Inhibitors on the Induction of Gene Expression by Long-Acting beta2-Adrenoceptor Agonists and Glucocorticoids
… proposed to enhance the clinical efficacy of PDE4 inhibitors. One of these is the use of dual PDE3/4 inhibitors, which in addition to providing superior anti-inflammatory activity when compared to a PDE4 inhibitor alone, will also promote bronchodilatation. The present study demonstrates that …
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Cyclic AMP modulation and its effects on chemo-resistant colon cancer cell proliferation and survival
… including inhibitors of phosphodiesterase 4 (PDE4) enzymes, which are under clinical development for other disease states, to inhibit the breakdown of cAMP and to assess the effects of raising intracellular cAMP on colon cancer proliferation and survival. I found that some chemo-resistant …
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Phosphodiesterase 4 inhibitors for the treatment of inflammation associated with respiratory disease
… on the selection of novel phosphodiesterase 4 (PDE4) inhibitors for the treatment of inflammation associated with respiratory diseases such as asthma and chronic obstructive pulmonary disease. A number of issues, relevant at the time, have been considered including: a) in vitro methods …
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Regulation of cAMP-Dependent Gene Expression in Airway Epithelial Cells: A Transcriptional and Pharmacodynamic Analysis
… agonist linked to an analogue of the PDE4 inhibitor, GSK 256066, by a pent-1-yn-1ylbenzene spacer. Pharmacodynamic studies established that the PDE4 inhibitor pharmacophore produced a 35.5-fold increase in affinity for the b2-adrenoceptor relative to the monofunctional parent compound …
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Role Of Gravin In Endothelial Wound Healing
… molecules including PKA-RII subunits, PKCα, PDE4, β2 adrenoreceptor and actin cytoskeleton. Initial characterization of gravin has revealed that this protein is undetectable in endothelia in vivo but expressed at the periphery of cultured endothelial cell (EC). Although the precise role of …
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The Role of Phosphodiesterases in Cyclic Nucleotide Compartmentation Across Different Pathways in the Adult Rat Ventricular Myocyte
… inhibitor, or Ro 20-1724 (10 µM) a selective PDE4 inhibitor. In myocytes treated with PGE2, unloaded cell shortening and intracellular calcium transients exhibited significantly different (p<0.05) values of 147 ± 10% and 138 ± 5% of pre-treatment (t=0) values, respectively, in the presence of …
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Functional characterization of Phosphodiesterase-4A in behavior and obesity
… In particular, one member of this family termed PDE4 is highly expressed in regions of the brain that may play a role in these psychiatric disorders such as the prefrontal cortex (PFC), hippocampus, amygdala, and striatum. PDE4 has four subtypes (A, B, C, and D), of which only PDE4C is not highly …
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Regulation of cAMP Signalling to Phospholemman by Phosphodiesterases
… subtypes 2-4 in biochemical assays identified PDE4 as the predominant PDE involved in modulating PLM phosphorylation at Ser68, the consensus PKA site, in the presence of the β-AR agonist isoprenaline hydrochloride (ISO). The augmentation of PLM-Ser68 phosphorylation was accompanied by a …
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Adrenergic Mobilization of the Immune System and the Anti-Cancer Effects of Exercise
… while β1-AR blockade or β1-AR blockade plus PDE4 inhibition significantly augment the mobilization of NK-cells or monocytes, γδ T-cells, and CD8 T-cells, respectively. We provide single cell transcriptomic data to further the understanding of signaling within immune cells during exercise, and …
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Efeito relaxante de derivados N-sulfonilidrazônicos do rolipram em traqueia de cobaia : investigação do mecanismo de ação do LASSBio-1846
… symptoms of airway diseases were synthesized new PDE4 inhibitors from rolipram. The new N - sulfonilhidrazone derivatives had been only tested on in vitro enzymatic assa ys. To investigate their effects on physiological conditions, the guinea - pig trachea model was selected. Thus, the present …
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Potential Natural Product Phosphodiesterase Inhibitors
… Third, a new synthesis of psychoactive PDE4 inhibitor was attempted. An in silico screen was performed using chemical structures of isolated compounds thought to have some PDE inhibitory activity based on traditional use of the plants. A collection of compounds with structures similar to …
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Aberrant assembly and function of a hippocampal circuit in a genetic mouse model of schizophrenia
… a link between Disc1 and the phosphodiesterase, PDE4B, which is important for the degradation of cAMP. Disc1Tm1Kara mutant mice also have decreases in levels of many isoforms of PDE4 as well as increases in cAMP and its downstream target pCREB. Finally, Nrp1 and Sema3A, guidance cues that are …
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Sex differences in the cardiac beta-adrenergic receptor contractile response
… protein, G<sub>i-2</sub>á protein, PDE4D, PP1 or PP2A as determined with western blotting. Adenylyl cyclase V/VI was expressed in significantly higher levels in female myocytes. Females showed enhanced cAMP accumulation upon ISO treatment with and without PDE4 inhibition. No sex …
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The Role of Cdk5 in the Regulation of Dopamine Neurotransmission, Neuronal Excitability, and Reward-Related Behavior
… sites on cAMP-specific phosphodiesterase 4 (PDE4), an important modulator of PKA signaling. These antibodies to Ser53 PDE4D3 (PKA site) and pSer573 PDE4D3 (ERK site) provide insight into the crosstalk between PKA and ERK pathways in the regulation of cAMP. Finally, we identified and confirmed …
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The crosstalk between the ERK and the cAMP signalling pathways in PC12 Cells
… combination of both cilostamide and rolipram (a PDE4 inhibitor) turned the proliferative effect of EGF into a differentiation effect. The route for cAMP in the regulation of the ERK pathway was decomposed by using the cAMP analogues 8-pCPT-2’-O-Me-cAMP and 6-Bnz-cAMP. They specifically activate …