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Year Number of Results
1990 1
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68 results

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Cyclic adenosine monophosphate/phosphodiesterase 4 pathway associated with immune infiltration and PD-L1 expression in lung adenocarcinoma cells.
Tong L, Shan M, Zou W, Liu X, Felsher DW, Wang J. Tong L, et al. Front Oncol. 2022 Aug 1;12:904969. doi: 10.3389/fonc.2022.904969. eCollection 2022. Front Oncol. 2022. PMID: 35978822 Free PMC article.
In the cell experiment, forskolin (an adenylate cyclase activator) and zardaverine (a PDE4 inhibitor) enhance the cAMP pathway and decrease PD-L1 expression, while SQ2253 (an adenylate cyclase inhibitor) inhibits the cAMP pathway and increases PD-L1 expression of the LUAD …
In the cell experiment, forskolin (an adenylate cyclase activator) and zardaverine (a PDE4 inhibitor) enhance the cAMP pathway and de …
Inhibition of Recruitment and Activation of Neutrophils by Pyridazinone-Scaffold-Based Compounds.
Moniot A, Braux J, Siboni R, Guillaume C, Audonnet S, Allart-Simon I, Sapi J, Tirouvanziam R, Gérard S, Gangloff SC, Velard F. Moniot A, et al. Int J Mol Sci. 2022 Jun 29;23(13):7226. doi: 10.3390/ijms23137226. Int J Mol Sci. 2022. PMID: 35806233 Free PMC article.
Compound 4ba and zardaverine were tested in vivo for their ability to limit tissue recruitment of PMNs in a murine air pouch model. ...Using a lung inflammation model, we proved that PMNs transmigration led to reduced expression of the CD16 phagocytic receptor, which was s …
Compound 4ba and zardaverine were tested in vivo for their ability to limit tissue recruitment of PMNs in a murine air pouch model. . …
Insights into the potential of withanolides as Phosphodiesterase-4 (PDE4D) inhibitors.
Rathi A, Kumar V, Sundar D. Rathi A, et al. J Biomol Struct Dyn. 2023 Apr;41(6):2108-2117. doi: 10.1080/07391102.2022.2028679. Epub 2022 Jan 21. J Biomol Struct Dyn. 2023. PMID: 35060432
These compounds had a better binding affinity and similar interactions as that of an already known inhibitor (Zardaverine) of PDE4D. These results warrant further in-vitro and in-vivo investigations to examine their therapeutic potential as an inhibitor of PDE4D.Communicat …
These compounds had a better binding affinity and similar interactions as that of an already known inhibitor (Zardaverine) of PDE4D. …
Pharmacological and molecular dynamics analyses of differences in inhibitor binding to human and nematode PDE4: Implications for management of parasitic nematodes.
Schuster KD, Mohammadi M, Cahill KB, Matte SL, Maillet AD, Vashisth H, Cote RH. Schuster KD, et al. PLoS One. 2019 Mar 27;14(3):e0214554. doi: 10.1371/journal.pone.0214554. eCollection 2019. PLoS One. 2019. PMID: 30917179 Free PMC article.
We observed that roflumilast (human PDE4-selective inhibitor) and zardaverine (selective for human PDE3 and PDE4) were 159- and 77-fold less potent, respectively, in inhibiting C. elegans PDE4. ...Of 32 residues within 5 A of the ligand binding site, five revealed signific …
We observed that roflumilast (human PDE4-selective inhibitor) and zardaverine (selective for human PDE3 and PDE4) were 159- and 77-fo …
A Dual Phosphodiesterase Inhibitor, Zardaverine (Type 3/4), Enhances Motility of Frozen-thawed Boar Sperm.
Jeong J, Sa SJ, Chung H, Baek S, Choi I. Jeong J, et al. Cryo Letters. 2018 May/Jun;39(3):196-200. Cryo Letters. 2018. PMID: 30059566
The kinetic values were significantly higher with the 50 uM Zardaverine supplementation compared to non-treated control. Furthermore, there were no toxic effects of the Zardaverine treatment. CONCLUSION: The dual phosphodiesterase inhibitor (type 3/4) Zardaverine
The kinetic values were significantly higher with the 50 uM Zardaverine supplementation compared to non-treated control. Furthermore, …
Targeting tumor cells based on Phosphodiesterase 3A expression.
Nazir M, Senkowski W, Nyberg F, Blom K, Edqvist PH, Jarvius M, Andersson C, Gustafsson MG, Nygren P, Larsson R, Fryknäs M. Nazir M, et al. Exp Cell Res. 2017 Dec 15;361(2):308-315. doi: 10.1016/j.yexcr.2017.10.032. Epub 2017 Oct 26. Exp Cell Res. 2017. PMID: 29107068
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. ...
Cell lines with high PDE3A expression showed marked in vitro sensitivity to PDE inhibitors zardaverine and quazinone, when compared w …
Cytotoxicity of Zardaverine in Embryonal Rhabdomyosarcoma from a Costello Syndrome Patient.
Cartledge DM, Robbins KM, Drake KM, Sternberg R, Stabley DL, Gripp KW, Kolb EA, Sol-Church K, Napper AD. Cartledge DM, et al. Front Oncol. 2017 Apr 3;7:42. doi: 10.3389/fonc.2017.00042. eCollection 2017. Front Oncol. 2017. PMID: 28421158 Free PMC article.
Many PDE inhibitors in addition to zardaverine were tested on CS242 ERMS, but almost all had no effect. ...Two recent studies presented possible mechanistic explanations for the cytotoxicity of zardaverine in HeLa cells. One revealed that zardaverine inhibite …
Many PDE inhibitors in addition to zardaverine were tested on CS242 ERMS, but almost all had no effect. ...Two recent studies present …
Design and synthesis of 4,5,6,7-tetrahydro-1H-1,2-diazepin-7-one derivatives as a new series of Phosphodiesterase 4 (PDE4) inhibitors.
Guariento S, Karawajczyk A, Bull JA, Marchini G, Bielska M, Iwanowa X, Bruno O, Fossa P, Giordanetto F. Guariento S, et al. Bioorg Med Chem Lett. 2017 Jan 1;27(1):24-29. doi: 10.1016/j.bmcl.2016.11.040. Epub 2016 Nov 16. Bioorg Med Chem Lett. 2017. PMID: 27890378
The resulting compounds demonstrated PDE4 inhibitory activity in cell free and cell-based assays comparable to the Zardaverine control used, suggesting potential avenues for their further development....
The resulting compounds demonstrated PDE4 inhibitory activity in cell free and cell-based assays comparable to the Zardaverine contro …
Multi-omics "upstream analysis" of regulatory genomic regions helps identifying targets against methotrexate resistance of colon cancer.
Kel AE, Stegmaier P, Valeev T, Koschmann J, Poroikov V, Kel-Margoulis OV, Wingender E. Kel AE, et al. EuPA Open Proteom. 2016 Sep 9;13:1-13. doi: 10.1016/j.euprot.2016.09.002. eCollection 2016 Dec. EuPA Open Proteom. 2016. PMID: 29900117 Free PMC article.
We identified the following potential drug targets against induced resistance of cancer cells towards chemotherapy by methotrexate (MTX): TGFalpha, IGFBP7, alpha9-integrin, and the following chemical compounds: zardaverine and divalproex as well as human metabolites such a …
We identified the following potential drug targets against induced resistance of cancer cells towards chemotherapy by methotrexate (MTX): TG …
68 results