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Journal articles on the topic 'Phosphodiesterase 4 (PDE -4) inhibitors'

Author: Grafiati

Published: 5 June 2025

Last updated: 2 August 2025

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1

Germain, Nöella, Elisabeth Boichot, Jean-Michel Planquois, and Vincent Lagente. "Reduced Airway Hyperresponsiveness by Phosphodiesterase 3 and 4 Inhibitors in Guinea-Pigs." Mediators of Inflammation 8, no. 3 (1999): 153–57. http://dx.doi.org/10.1080/09629359990487.

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The aim of the present study was to compare the effects of selective phosphodiesterase (PDE) 3, 4 and 5 inhibitors on antigen-induced airway hyperresponsiveness in sensitized guinea-pigs. When the sensitized guinea-pigs were orally pre-treated with the selective PDE4 inhibitor, Ro 20-1724 (30 mg/kg), and studied 48 h after OA, a significant reduction (p<0.01) of the leftward shift of the dose-response curve to ACh was noted, whereas it was ineffective at the lower dose (10 mg/kg). Administration of the selective PDE3 inhibitor, milrinone (30 mg/kg) also elicited a significant reduction (p&l

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2

Ghavami, Afshin, Warren D. Hirst, and Thomas J. Novak. "Selective Phosphodiesterase (PDE)-4 Inhibitors." Drugs in R & D 7, no. 2 (2006): 63–71. http://dx.doi.org/10.2165/00126839-200607020-00001.

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3

Sarfati, Marika, Véronique Mateo, Sylvie Baudet, et al. "Sildenafil and vardenafil, types 5 and 6 phosphodiesterase inhibitors, induce caspase-dependent apoptosis of B-chronic lymphocytic leukemia cells." Blood 101, no. 1 (2003): 265–69. http://dx.doi.org/10.1182/blood-2002-01-0075.

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Abstract Type 4 phosphodiesterase (PDE4) inhibitors reportedly induce apoptosis in chronic lymphocytic leukemia (CLL) cells. Following clinical improvement of one previously untreated CLL patient with sildenafil therapy, we evaluated the in vitro induction of apoptosis in CLL cells by 4 PDE5/6 inhibitors, including sildenafil, vardenafil, zaprinast, and methoxyquinazoline (MQZ). After 24 hours of culture, the various PDE inhibitors differed in their ability to induce apoptosis, with zaprinast displaying no killing effect. Normal B cells isolated from control donors were totally resistant to PD

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4

Phillips, Peter G., Lu Long, Martin R. Wilkins, and Nicholas W. Morrell. "cAMP phosphodiesterase inhibitors potentiate effects of prostacyclin analogs in hypoxic pulmonary vascular remodeling." American Journal of Physiology-Lung Cellular and Molecular Physiology 288, no. 1 (2005): L103—L115. http://dx.doi.org/10.1152/ajplung.00095.2004.

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We investigated the effects of prostacyclin analogs and isoform-selective phosphodiesterase (PDE) inhibitors, alone and in combination, on pulmonary vascular remodeling in vitro and in vivo. Vascular smooth muscle cells (VSMC) isolated from pulmonary (proximal and distal) and systemic circulations demonstrated subtle variations in expression of PDE isoform mRNA. However, using biochemical assays, we found PDE3 and PDE4 isoforms to be responsible for the majority of cAMP hydrolysis in all VSMC. In growth assays, the prostacyclin analogs cicaprost and iloprost inhibited mitogen-induced prolifera

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Schick, Martin Alexander, and Nicolas Schlegel. "Clinical Implication of Phosphodiesterase-4-Inhibition." International Journal of Molecular Sciences 23, no. 3 (2022): 1209. http://dx.doi.org/10.3390/ijms23031209.

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The pleiotropic function of 3′,5′-cyclic adenosine monophosphate (cAMP)-dependent pathways in health and disease led to the development of pharmacological phosphodiesterase inhibitors (PDE-I) to attenuate cAMP degradation. While there are many isotypes of PDE, a predominant role of PDE4 is to regulate fundamental functions, including endothelial and epithelial barrier stability, modulation of inflammatory responses and cognitive and/or mood functions. This makes the use of PDE4-I an interesting tool for various therapeutic approaches. However, due to the presence of PDE4 in many tissues, there

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6

Cheng, Jingfei, Michael A. Thompson, Henry J. Walker, et al. "Differential regulation of mesangial cell mitogenesis by cAMP phosphodiesterase isozymes 3 and 4." American Journal of Physiology-Renal Physiology 287, no. 5 (2004): F940—F953. http://dx.doi.org/10.1152/ajprenal.00079.2004.

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Mesangial cell (MC) mitogenesis is regulated through “negative cross talk” between cAMP-PKA and ERK signaling. Although it is widely accepted that cAMP inhibits mitogenesis through PKA-mediated phosphorylation of Raf-1, recent studies have indicated that cAMP-mediated inhibition of mitogenesis may occur independently of Raf-1 phosphorylation or without inhibiting ERK activity. We previously showed that MCs possess functionally compartmentalized intracellular pools of cAMP that are differentially regulated by cAMP phosphodiesterases (PDE); an intracellular pool directed by PDE3 but not by PDE4

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7

Kopanitsa, Liliya, Maksym V. Kopanitsa, Dewi Safitri, Graham Ladds, and David S. Bailey. "Suppression of Proliferation of Human Glioblastoma Cells by Combined Phosphodiesterase and Multidrug Resistance-Associated Protein 1 Inhibition." International Journal of Molecular Sciences 22, no. 18 (2021): 9665. http://dx.doi.org/10.3390/ijms22189665.

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The paucity of currently available therapies for glioblastoma multiforme requires novel approaches to the treatment of this brain tumour. Disrupting cyclic nucleotide-signalling through phosphodiesterase (PDE) inhibition may be a promising way of suppressing glioblastoma growth. Here, we examined the effects of 28 PDE inhibitors, covering all the major PDE classes, on the proliferation of the human U87MG, A172 and T98G glioblastoma cells. The PDE10A inhibitors PF-2545920, PQ10 and papaverine, the PDE3/4 inhibitor trequinsin and the putative PDE5 inhibitor MY-5445 potently decreased glioblastom

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8

Sherpa, Rinzhin T., Cynthia J. Koziol-White, and Reynold A. Panettieri. "Advancing Obstructive Airway Disease Treatment: Dual PDE3/4 Inhibition as a Therapeutic Strategy." Cells 14, no. 9 (2025): 659. https://doi.org/10.3390/cells14090659.

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Obstructive airway diseases, including asthma and chronic obstructive pulmonary disease (COPD), evoke significant global health concerns manifested by airway inflammation and obstruction. Despite their differing origins, shared pathophysiological features and responses to therapeutic interventions highlight common molecular mechanisms. Standard treatments include inhaled bronchodilators, with combination therapies offering enhanced symptom control. Cyclic AMP (cAMP) plays a crucial role in airway relaxation. Phosphodiesterase (PDE) decreases cAMP levels, thereby attenuating the relaxation of a

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9

Organtzis, John, Sofia Lampaki, Paul Zarogoulidis, et al. "Phosphodiesterase (PDE)-4 Inhibitors and COPD Correlation with Cancer." Journal of Cancer 5, no. 8 (2014): 625–27. http://dx.doi.org/10.7150/jca.9730.

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10

Neumann, Joachim, Rafaela Voss, Ulrich Laufs, Christian Werner, and Ulrich Gergs. "Phosphodiesterases 2, 3 and 4 can decrease cardiac effects of H2-histamine-receptor activation in isolated atria of transgenic mice." Naunyn-Schmiedeberg's Archives of Pharmacology 394, no. 6 (2021): 1215–29. http://dx.doi.org/10.1007/s00210-021-02052-y.

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AbstractHistamine exerts cAMP-dependent positive inotropic effects (PIE) and positive chronotropic effects (PCE) on isolated left and right atria, respectively, of transgenic mice which overexpress the human H2-receptor in the heart (=H2-TG). To determine whether these effects are antagonized by phosphodiesterases (PDEs), contractile studies were done in isolated left and right atrial preparations of H2-TG. The contractile effects of histamine were tested in the additional presence of the PDE-inhibitorserythro-9-(2-hydroxy-3-nonyl)adenine hydrochloride (EHNA, 1 μM, PDE2-inhibitor) or cilostami

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11

Jiang, Wei, Xueyong Wang, Shan Li, Nan Li, Zhongwei Li, and Zhiguo Xu. "Advances in the Study of PDE4 Inhibitors in Dermatological Disorders." Academic Journal of Science and Technology 11, no. 1 (2024): 166–68. http://dx.doi.org/10.54097/a1y90g60.

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Since the 1980s, phosphodiesterase 4 (PDE-4) has been one of the most prominent targets for the treatment of inflammatory diseases. More recently, a number of synthetic ligands targeting PDE-4 have received more attention in the academic and pharmaceutical communities and are expected to have applications in these diseases. Due to various potential side effects of PDE-4 inhibitors, there are several obstacles to the clinical translation of specific PDE-4 inhibitors from the preclinical to the clinical phase. Therefore, similar to roflumilast in chronic obstructive pulmonary disease, many PDE-4

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12

Erdely, Aaron, Diane Kepka-Lenhart, Melissa Clark, et al. "Inhibition of phosphodiesterase 4 amplifies cytokine-dependent induction of arginase in macrophages." American Journal of Physiology-Lung Cellular and Molecular Physiology 290, no. 3 (2006): L534—L539. http://dx.doi.org/10.1152/ajplung.00326.2005.

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Arginase is greatly elevated in asthma and is thought to play a role in the pathophysiology of this disease. As inhibitors of phosphodiesterase 4 (PDE4), the predominant PDE in macrophages, elevate cAMP levels and reduce inflammation, they have been proposed for use in treatment of asthma and chronic obstructive pulmonary disease. As cAMP is an inducer of arginase, we tested the hypothesis that a PDE4 inhibitor would enhance macrophage arginase induction by key cytokines implicated in asthma and other pulmonary diseases. RAW 264.7 cells were stimulated with IL-4 or transforming growth factor (

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Turner, Mark J., Yishan Luo, David Y. Thomas, and John W. Hanrahan. "The dual phosphodiesterase 3/4 inhibitor RPL554 stimulates rare class III and IV CFTR mutants." American Journal of Physiology-Lung Cellular and Molecular Physiology 318, no. 5 (2020): L908—L920. http://dx.doi.org/10.1152/ajplung.00285.2019.

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Over 2,000 mutations have been reported in the cystic fibrosis transmembrane conductance regulator ( cftr) gene, many of which cause disease but are rare and have no effective treatment. Thus, there is an unmet need for new, mutation-agnostic therapies for cystic fibrosis (CF). Phosphodiesterase (PDE) inhibitors are one such class of therapeutics that have been shown to elevate intracellular cAMP levels and stimulate CFTR-dependent anion secretion in human airway epithelia; however, the number of people with CF that could be helped by PDE inhibitors remains to be determined. Here we used Fishe

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14

Teixeira, M. M., R. W. Gristwood, N. Cooper, and P. G. Hellewell. "Phosphodiesterase (PDE)4 inhibitors: anti-inflammatory drugs of the future?" Trends in Pharmacological Sciences 18, no. 5 (1997): 164–70. http://dx.doi.org/10.1016/s0165-6147(97)01049-3.

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Teixeira, Mauro M., Robert W. Gristwood, Nicola Cooper, and Paul G. Hellewell. "Phosphodiesterase (PDE)4 inhibitors: anti-inflammatory drugs of the future?" Trends in Pharmacological Sciences 18, no. 4 (1997): 164–70. http://dx.doi.org/10.1016/s0165-6147(97)90613-1.

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16

Kim, Doo Ho, and Adam Lerner. "Type 4 Cyclic Adenosine Monophosphate Phosphodiesterase as a Therapeutic Target in Chronic Lymphocytic Leukemia." Blood 92, no. 7 (1998): 2484–94. http://dx.doi.org/10.1182/blood.v92.7.2484.

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Abstract Theophylline, a drug known to inhibit several classes of adenosine 3′5′ cyclic monophosphate (cAMP) phosphodiesterases (PDEs), induces apoptosis in chronic lymphocytic leukemia (CLL) cells. Because the PDE target for theophylline in CLL remains unknown, we examined the ability of isoform-specific PDE inhibitors to increase cAMP levels and induce apoptosis in primary CLL cells. Reverse transcriptase-polymerase chain reaction of purified CLL cDNA amplified transcripts for PDE1B, 4A and 4B. The type 4 PDE inhibitor rolipram but not the type 1 inhibitor vinpocetine increased CLL cAMP leve

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Kim, Doo Ho, and Adam Lerner. "Type 4 Cyclic Adenosine Monophosphate Phosphodiesterase as a Therapeutic Target in Chronic Lymphocytic Leukemia." Blood 92, no. 7 (1998): 2484–94. http://dx.doi.org/10.1182/blood.v92.7.2484.2484_2484_2494.

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Theophylline, a drug known to inhibit several classes of adenosine 3′5′ cyclic monophosphate (cAMP) phosphodiesterases (PDEs), induces apoptosis in chronic lymphocytic leukemia (CLL) cells. Because the PDE target for theophylline in CLL remains unknown, we examined the ability of isoform-specific PDE inhibitors to increase cAMP levels and induce apoptosis in primary CLL cells. Reverse transcriptase-polymerase chain reaction of purified CLL cDNA amplified transcripts for PDE1B, 4A and 4B. The type 4 PDE inhibitor rolipram but not the type 1 inhibitor vinpocetine increased CLL cAMP levels. Rolip

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18

Temkitthawon, Prapapan, Kanokwan Changwichit, Nantaka Khorana, Jarupa Viyoch, Khanit Suwanborirux, and Kornkanok Ingkaninan. "Phenanthrenes from Eulophia macrobulbon as Novel Phosphodiesterase-5 Inhibitors." Natural Product Communications 12, no. 1 (2017): 1934578X1701200. http://dx.doi.org/10.1177/1934578x1701200121.

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Phosphodiesterase 5 (PDE5) inhibitors can be used for the treatment of erectile dysfunction and pulmonary hypertension. In order to search for new leads of PDE5 inhibitors, we investigated the chemical constituents of the tubers of Eulophia macrobulbon (E.C. Parish & Rchb. f) Hook. f A new phenanthrene, 9,10-dihydro-4-(4′-hydroxybenzyl)-2,5-dimethoxyphenanthrene-1,7-diol (1) and three known phenanthrenes i.e., 1-(4′-hydroxybenzyl)-4,8-dimethoxyphenanthrene-2,7-diol (2), (9,10-dihydro-2,5-dimethoxyphenanthrene-1,7-diol (3) and 1,5,7-trimethoxyphenanthrene-2,6-diol) (4) were isolated. Among

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19

Świerczek, Artur, Krzysztof Pociecha, Hanna Plutecka, Marietta Ślusarczyk, Grażyna Chłoń-Rzepa, and Elżbieta Wyska. "Pharmacokinetic/Pharmacodynamic Evaluation of a New Purine-2,6-Dione Derivative in Rodents with Experimental Autoimmune Diseases." Pharmaceutics 14, no. 5 (2022): 1090. http://dx.doi.org/10.3390/pharmaceutics14051090.

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Current treatment strategies of autoimmune diseases (ADs) display a limited efficacy and cause numerous adverse effects. Phosphodiesterase (PDE)4 and PDE7 inhibitors have been studied recently as a potential treatment of a variety of ADs. In this study, a PK/PD disease progression modeling approach was employed to evaluate effects of a new theophylline derivative, compound 34, being a strong PDE4 and PDE7 inhibitor. Activity of the studied compound against PDE1 and PDE3 in vitro was investigated. Animal models of multiple sclerosis (MS), rheumatoid arthritis (RA), and autoimmune hepatitis were

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20

Tausend, William, Paige Hoyer, Morgan Arnold, et al. "Successful Treatment of Vitiligo with Crisaborole 2% Ointment." SKIN The Journal of Cutaneous Medicine 3, no. 2 (2019): 111–13. http://dx.doi.org/10.25251/skin.3.2.47.

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Vitiligo is a common disorder of skin pigmentation resulting from autoimmune destruction of melanocytes. A variety of topical and systemic treatment options have been tried with varying success. Here we describe the case of a man with refractory vitiligo successfully treated with topical crisaborole ointment.Crisaborole ointment is a topical phosphodiesterase (PDE)-4 inhibitor recently FDA-approved for the treatment of atopic dermatitis. Previous literature has discussed the possible role of systemic PDE-4 inhibitors in vitiligo; herein, we discuss the ability of topical crisaborole to acceler

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21

Chao, Pin-Chun, and Kirk L. Hamilton. "Genistein stimulates electrogenic Cl− secretion via phosphodiesterase modulation in the mouse jejunum." American Journal of Physiology-Cell Physiology 297, no. 3 (2009): C688—C698. http://dx.doi.org/10.1152/ajpcell.00152.2009.

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Previously, we demonstrated that genistein stimulated Cl− secretion in the mouse jejunum (Baker MJ and Hamilton KL, Am J Physiol Cell Physiol 287: C1636–C1645, 2004); however, the mode of action of genistein still remains unclear. Here, we examined the activation of Cl− secretion by the modulation of phosphodiesterases (PDEs) by genistein (75 μM) in the mouse jejunum with the Ussing short-circuit current ( Isc) technique. Drugs tested included theophylline (10 mM), a nonspecific PDE inhibitor; 8-methoxymethyl-3-isobutyl-1-methylxanthine (8-MM-IBMX; 100 μM), erythro-9-(2-hydroxyl-3-nonyl)-adeni

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Crowley, Erika L., and Melinda J. Gooderham. "Phosphodiesterase-4 Inhibition in the Management of Psoriasis." Pharmaceutics 16, no. 1 (2023): 23. http://dx.doi.org/10.3390/pharmaceutics16010023.

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Psoriasis is a common chronic immune-mediated disease with many comorbidities and impacts on quality of life. Among the treatments for psoriasis, phosphodiesterase-4 (PDE4) inhibitors are emerging with expanding options. PDE4 inhibitors play a pivotal role in the inflammatory cascade by degrading cyclic adenosine monophosphate (cAMP), contributing to pro-inflammatory mediator production. Apremilast, an oral PDE4 inhibitor, is approved for psoriasis. While effective, its adverse effects can limit its utility. Roflumilast, a topical PDE4 inhibitor, was also recently approved for psoriasis and sh

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Ajmer Singh Grewal, Neelam Sharma, Sukhbir Singh, and Sandeep Arora. "In Silico Designing of Novel Thiazolidine-2-one Derivatives as Dual PDE4/7 Inhibitors for Inflammatory Disorders." Journal of Pharmaceutical Technology, Research and Management 5, no. 2 (2019): 149–62. http://dx.doi.org/10.15415/jptrm.2017.52010.

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Phosphodiesterase 4 (PDE4) and phosphodiesterase 7 (PDE7), members of PDE super family, catalyse metabolism of secondary messenger cyclic adenosine monophosphate leading to augmented inflammatory processes in pro-inflammatory and immune-modulatory cells. Dual inhibitors of PDE4/7 are a novel class of drug candidates which can regulate pro-inflammatory as well as function of immune T-cell and are particularly beneficial for the treatment of various inflammatory diseasesdevoid of unwanted actions. Intense efforts have been directed towards the development of effective dual inhibitors of both PDE

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Haynes, J., P. A. Kithas, A. E. Taylor, and S. J. Strada. "Selective inhibition of cGMP-inhibitable cAMP phosphodiesterase decreases pulmonary vasoreactivity." American Journal of Physiology-Heart and Circulatory Physiology 261, no. 2 (1991): H487—H492. http://dx.doi.org/10.1152/ajpheart.1991.261.2.h487.

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Guanosine 3',5'-cyclic monophosphate (cGMP) and adenosine 3',5'-cyclic monophosphate (cAMP) are mediators of smooth muscle relaxation. In this study, selective inhibitors of phosphodiesterase (PDE) isozymes were used to assess the role of cyclic nucleotide hydrolysis in angiotensin II (ANG II) and hypoxic pulmonary vasoconstriction. In isolated rat lungs, the hypoxic pressor response (HPR) was induced with a 95% N2-5% CO2 gas mixture. When administered during the plateau of the HPR, trequinsin (nonselective PDE inhibitor) and indolidan (cGMP-inhibitable cAMP PDE inhibitor) significantly (P = 0

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Fournier, Valérie, Pierre Leclerc, Nathaly Cormier, and Janice L. Bailey. "Implication of Calmodulin‐Dependent Phosphodiesterase Type 1 During Bovine Sperm Capacitation." Journal of Andrology 24, no. 1 (2003): 104–12. http://dx.doi.org/10.1002/j.1939-4640.2003.tb02648.x.

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ABSTRACT: Phosphodiesterases (PDEs) are enzymes that degrade cyclic nucleotides. The calcium‐calmodulin dependent PDE type 1 (PDE 1) and the cyclic adenosine monophosphate (cAMP)‐specific PDE type 4 (PDE 4) have been implicated in sperm function. We tested the hypothesis that specific PDEs regulate capacitation of bovine sperm in a manner independent of those that mediate motility. Our objectives were to determine the effects of inhibiting PDE 1 and PDE 4 on capacitation and motility, and to compare these effects to those of heparin, which is necessary for capacitation of bull sperm in vitro.

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Rickles, Richard J., Laura T. Pierce, Thomas P. Giordano, et al. "Adenosine A2A receptor agonists and PDE inhibitors: a synergistic multitarget mechanism discovered through systematic combination screening in B-cell malignancies." Blood 116, no. 4 (2010): 593–602. http://dx.doi.org/10.1182/blood-2009-11-252668.

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Abstract Using a combination high-throughput screening technology, multiple classes of drugs and targeted agents were identified that synergize with dexamethasone (Dex) in multiple myeloma (MM) cells. Performing combination screening with these enhancers, we discovered an unexpected synergistic interaction between adenosine receptor agonists and phosphodiesterase (PDE) inhibitors that displays substantial activity in a panel of MM and diffuse large B-cell lymphoma (DLBCL) cell lines and tumor cells from MM patients. We have used selective adenosine receptor agonists, antagonists, and PDE inhib

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Sugiyama, Takuji, Yuji Narukawa, Shunsuke Shibata, Ryo Masui, and Fumiyuki Kiuchi. "New 2-(2-Phenylethyl)chromone Derivatives and Inhibitors of Phosphodiesterase (PDE) 3A from Agarwood." Natural Product Communications 11, no. 6 (2016): 1934578X1601100. http://dx.doi.org/10.1177/1934578x1601100624.

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The MeOH extract of agarwood showed inhibitory activity against phosphodiesterase (PDE) 3A. Fractionation of the extract led to the isolation of two new 2-(2-phenylethyl)chromones, 6,8-dihydroxy-2-[2-(4′-methoxyphenyl)ethyl]chromone (6), and 6,7-dihydroxy-2-(2-phenylethyl)chromone (8), together with six known compounds. All isolated compounds were tested for their PDE 3A inhibitory activity using fluorescence polarization method. Compound 7 showed PDE 3 A inhibitory activity with IC50 of 4.83 μM.

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Akisheva, A. S., V. B. Larionov, M. Y. Golovenko та ін. "In silico exploration of antinociceptive activity of 1,4-benzodiazepines: Molecular docking on α1 A-adrenoceptor, and phosphodiesterase 4". Regulatory Mechanisms in Biosystems 15, № 2 (2024): 327–36. http://dx.doi.org/10.15421/022447.

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Recently, scientists have established that several benzodiazepines were found to enhance the activation of a cAMP response element pathway by α1A-adrenergic receptors, but this effect was attributed to off-target inhibition of phosphodiesterases 4. The study explores the pain-relief potential of 1,4-benzodiazepines using in silico methods, focusing on their interaction with α1A-adrenoceptors (α1-AR) and phosphodiesterase 4 (PDE4). AutoDock Vina-1.2.5 and Glide (Schrödinger Suite) (2023-2) were used to calculate the binding affinities and determine the features of their interactions by the mole

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Teng, Bunyan, Daniel N. Darlington, and Andrew P. Cap. "Adenosine Regulation of cAMP through Phosphodiesterases." Blood 132, Supplement 1 (2018): 2424. http://dx.doi.org/10.1182/blood-2018-99-114929.

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Abstract Introduction: Adenosine, an autacoid and metabolite of ATP, has been known to have anti-platelet properties. Of the 4 adenosine receptors (ARs), only A2A AR have been implicated in adenosines anti-platelet properties in human. A2A AR is a G-Protein Coupled Receptors associated with a stimulatory G-Protein (Gs) that can activate adenylyl cyclase (AC) and increase intracellular cAMP. An elevation of cAMP has been shown to inhibit platelet aggregation to natural stimuli. Regulation of intracellular cAMP is balanced between synthesis by adenylate cyclase and degradation by phosphdiesteras

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Zhao, Hong, John Quilley, David C. Montrose, Swarna Rajagopalan, Qizhi Guan, and Carolyn J. Smith. "Differential effects of phosphodiesterase PDE-3/PDE-4-specific inhibitors on vasoconstriction and cAMP-dependent vasorelaxation following balloon angioplasty." American Journal of Physiology-Heart and Circulatory Physiology 292, no. 6 (2007): H2973—H2981. http://dx.doi.org/10.1152/ajpheart.00419.2006.

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It is known that cAMP and cGMP are important for vasorelaxation, and cyclic nucleotide phosphodiesterases (PDEs) regulate their levels. Balloon angioplasty (BAL) is associated with reduced cAMP and cGMP levels, and inhibition of PDE-3 reduces restenosis. In this study, we found that BAL increased PDE-3 activity, which affected vasoreactivity of rat aortic rings 24-h post-BAL; these were compared with intact (INT) and ex vivo endothelium-denuded rings (RUB) from sham rats. In BAL and RUB rings, vasorelaxant responses to ACh were abolished. The EC50 for phenylephrine (PE) was 1.8-fold less in RU

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McKenna, Sean D., Michael Pietropaolo, Enrico Gillio Tos, et al. "Pharmacological Inhibition of Phosphodiesterase 4 Triggers Ovulation in Follicle-Stimulating Hormone-Primed Rats." Endocrinology 146, no. 1 (2005): 208–14. http://dx.doi.org/10.1210/en.2004-0562.

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Phosphodiesterases (PDEs) are a family of enzymes that hydrolyze cyclic nucleotides to render them biologically inactive. As such, these enzymes are critical regulators of signal transduction pathways that use cyclic nucleotides as second messengers. PDE4 is one such member that has been identified in ovarian tissue and purported to have a role in the regulation of gonadotropin action. In the present study, selective PDE4 inhibitors enhanced intracellular signaling in a human LH receptor-expressing granulosa cell line. In vivo, PDE4 inhibition in FSH-primed rats resulted in ovulation, indicati

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Maiga, Mariama C., Bintou Ahmadou Ahidjo, Mamoudou Maiga, and William R. Bishai. "Roflumilast, a Type 4 Phosphodiesterase Inhibitor, Shows Promising Adjunctive, Host-Directed Therapeutic Activity in a Mouse Model of Tuberculosis." Antimicrobial Agents and Chemotherapy 59, no. 12 (2015): 7888–90. http://dx.doi.org/10.1128/aac.02145-15.

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ABSTRACTWith phosphodiesterase inhibitors (PDE-Is) showing significant promise in shortening tuberculosis treatment, we assessed the effect of roflumilast, an FDA-approved type 4 PDE-I, in both acute and chronic murine models of tuberculosis. Alone, roflumilast had no effect on lung bacillary burden and mortality. However, when roflumilast was used in combination with isoniazid, a reduction in lung bacillary burden was observed. These data suggest that roflumilast may be a good candidate for tuberculosis host-directed therapy (HDT).

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Essayan, D. M., S. K. Huang, B. J. Undem, A. Kagey-Sobotka, and L. M. Lichtenstein. "Modulation of antigen- and mitogen-induced proliferative responses of peripheral blood mononuclear cells by nonselective and isozyme selective cyclic nucleotide phosphodiesterase inhibitors." Journal of Immunology 153, no. 8 (1994): 3408–16. http://dx.doi.org/10.4049/jimmunol.153.8.3408.

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Abstract Cyclic nucleotide phosphodiesterase (PDE) enzymes are felt to play a role in the regulation of inflammatory responses through their effects on cAMP. In this study, we investigated the effects of nonselective and isozyme selective PDE inhibitors on the proliferative responses of peripheral blood mononuclear cells (PBMCs) to ragweed (RW, a Th2 stimulus), tetanus toxoid (TT, a Th1 stimulus), and phytohemagglutinin in ragweed-allergic patients. The nonselective PDE inhibitor 3-isobutyl-1-methylxanthine (IBMX) produced nearly identical concentration-dependent inhibition for PBMCs cultured

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Favot, Laure, Thérèse Keravis, Vincent Holl, Alain Bec, and Claire Lugnier. "VEGF-induced HUVEC migration and proliferation are decreased by PDE2 and PDE4 inhibitors." Thrombosis and Haemostasis 90, no. 08 (2003): 334–43. http://dx.doi.org/10.1160/th03-02-0084.

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SummaryMigration and proliferation of endothelial cells in response to VEGF play an important role in angiogenesis associated to pathologies such as atherosclerosis, diabetes and tumor development. Elevation of cAMP in endothelial cells has been shown to inhibit growth factor-induced proliferation. Our hypothesis was that inactivation of cAMP-specific phosphodiesterases (PDEs) would inhibit angiogenesis. The purpose of this study was to evaluate the effect of PDE inhibitors on in vitro and in vivo angiogenesis, using human umbilical vein endothelial cell (HUVEC) and chick chorioallantoic membr

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Rickles, Richard J., Laura Pierce, Thomas Giordano, et al. "Adenosine A2A Receptor Agonism and PDE Inhibition: A Synergistic Multi-Target Mechanism Discovered through Systematic Combination Screening in Multiple Myeloma." Blood 112, no. 11 (2008): 847. http://dx.doi.org/10.1182/blood.v112.11.847.847.

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Abstract Using a combination high throughput screening technology, we have discovered an unexpected synergistic interaction between adenosine A2A receptor (A2A) agonism and phosphodiesterase (PDE) inhibition that displays substantial activity in preclinical Multiple Myeloma (MM) models. High throughput combination screening allows the systematic testing of combinations of approved drugs and other biologically active molecules in cell based assays of tumor cell proliferation and viability. In this approach we generate a dose matrix for each chemical combination, capturing the combined activity

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Souness, John E., David Aldous, and Carol Sargent. "Immunosuppressive and anti-inflammatory effects of cyclic AMP phosphodiesterase (PDE) type 4 inhibitors." Immunopharmacology 47, no. 2-3 (2000): 127–62. http://dx.doi.org/10.1016/s0162-3109(00)00185-5.

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Smith, Carolyn J., Jing He, Jia-Zhen Ding, et al. "Uupregulation of High Affinity Cyclic AMP Phosphodiesterase (PDE) Genes Following BALloon Catheter Deendothelialization (Bal) in Rat Aorta." Hypertension 36, suppl_1 (2000): 706. http://dx.doi.org/10.1161/hyp.36.suppl_1.706-d.

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P75 Inhibitors of PDE 3 and/or PDE4 block smooth muscle cell (SMC) proliferation/migration in vitro and reduce restenosis. To evaluate chronic regulation of SMC PDEs, rats were subjected to BAL. At several times after BAL (30 min to 10days/10D), medial SMC were isolated from the thoracic aortae. Tissues were fractionated for total RNA (analyzed by Northern blots/ RNAase protection) or cytosolic protein (Western blots or low Km [100 nM] cAMP PDE activity). BAL-dependent increases in PDE4B mRNA were biphasic: 2.7-fold at 1hr, which declined by 24hr below control values, followed by 2-3-fold incr

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Al Matni, Mohammed Yaman, Lucille Meliton, Steven M. Dudek, and Eleftheria Letsiou. "Dual Inhibition of Phosphodiesterase 3 and 4 Enzymes by Ensifentrine Protects against MRSA-Induced Lung Endothelial and Epithelial Dysfunction." Cells 13, no. 21 (2024): 1750. http://dx.doi.org/10.3390/cells13211750.

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Acute Respiratory Distress Syndrome (ARDS) is a severe lung condition with a high mortality rate for which there are no effective therapeutics. The failure of the alveolar–capillary barrier, composed of lung endothelial (EC) and alveolar epithelial (AEC) cells, is a critical factor leading to excessive inflammation and edema characteristic of acute lung injury (ALI) pathophysiology. Phosphodiesterases (PDE) are enzymes well-recognized for their roles in regulating endothelial permeability and inflammation. Although PDE inhibitors are used as therapeutics for inflammatory diseases like COPD (ch

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Sharma, Himanshu, Viney Lather, Ajmer Singh Grewal, and Deepti Pandita. "Synthesis, Anti-inflammatory Activity and Docking Studies of Some Newer 1,3-Thiazolidine-2,4-dione Derivatives as Dual Inhibitors of PDE4 and PDE7." Current Computer-Aided Drug Design 15, no. 3 (2019): 225–34. http://dx.doi.org/10.2174/1573409914666181003151528.

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<P>Background: Phosphodiesterase 4 (PDE4) and phosphodiesterase 7 (PDE7), PDE superfamily members, increase inflammatory processes in immunomodulatory as well as pro-inflammatory cells via breakdown of cyclic adenosine monophosphate. Dual inhibitors of PDE4 and PDE7 are a novel class of drug candidates which can regulate pro-inflammatory as well as T-cell function and can be particularly advantageous in the treatment of a wide-ranging disorders associated with the immune system as well as inflammatory diseases with fewer unwanted adverse effects. Objective: The current research work was

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Reeves, M. L., B. K. Leigh, and P. J. England. "The identification of a new cyclic nucleotide phosphodiesterase activity in human and guinea-pig cardiac ventricle. Implications for the mechanism of action of selective phosphodiesterase inhibitors." Biochemical Journal 241, no. 2 (1987): 535–41. http://dx.doi.org/10.1042/bj2410535.

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Four cyclic nucleotide phosphodiesterase (PDE) activities were separated from low-speed supernatants of homogenates of human cardiac ventricle by DEAE-Sepharose chromatography, and designated PDE I-PDE IV in order of elution with an increasing salt gradient. PDE I was a Ca2+/calmodulin-stimulated activity, and PDE II was an activity with a high Km for cyclic AMP which was stimulated by low concentrations of cyclic GMP. Human ventricle PDE III had Km values of 0.14 microM (cyclic AMP) and 4 microM (cyclic GMP), and showed simple Michaelis-Menten kinetics with both substrates. PDE IV is a previo

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Sato, Yukio, Shyoko Sato, Tatsuo Yamamoto, Shigemi Ishikawa, Masataka Onizuka, and Yuzuru Sakakibara. "Phosphodiesterase type 4 inhibitor reduces the retention of polymorphonuclear leukocytes in the lung." American Journal of Physiology-Lung Cellular and Molecular Physiology 282, no. 6 (2002): L1376—L1381. http://dx.doi.org/10.1152/ajplung.00433.2001.

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Phosphodiesterase (PDE) type 4 is the predominant PDE isozyme in polymorphonuclear leukocytes (PMN) and plays a key role in the regulation of PMN activation. The aim of this study was to examine the effect of a PDE type 4 inhibitor, rolipram, on the functional changes and the retention of PMN in the lung. In vitro, F-actin content and L-selectin and CD11b expression of PMN stimulated by N-formyl-Met-Leu-Phe were measured by flow cytometry. PMN deformability was evaluated using silicon microchannels. Rolipram reduced the increase of F-actin and CD11b but did not change the decrease of L-selecti

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Liu, Ye-Na, Yi-You Huang, Jing-Mei Bao, et al. "Natural phosphodiesterase-4 (PDE4) inhibitors from Crotalaria ferruginea." Fitoterapia 94 (April 2014): 177–82. http://dx.doi.org/10.1016/j.fitote.2014.02.010.

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Doherty, Dearbhla, Ellie Karampini, Ciara Byrne, et al. "Targeted Inhibition of Phosphodiesterase (PDE) 4 As a Novel Therapy to Increase Endothelial Cell cAMP and Trigger Weibel Palade Body Exocytosis." Blood 142, Supplement 1 (2023): 3975. http://dx.doi.org/10.1182/blood-2023-178581.

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Background Desmopressin (DDAVP) is widely used in the treatment of VWD and other bleeding disorders. DDAVP activates V2 receptors (V2R) on endothelial cells (EC) to stimulate cAMP generation and Weibel-Palade body (WPB) exocytosis. However, DDAVP has inherent limitations, including lack of oral formulation, side-effects related to renal V2R agonism and sub-optimal responses in some patients. Aims To identify previously approved drugs with capacity to trigger cAMP-dependent WPB secretion in EC to repurpose as novel hemostatic therapeutic agents. Methods Candidate agents were identified by mecha

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Hütten, Matthias Christian, Tim Brokken, Helene Widowski, et al. "Acute Lung Functional and Airway Remodeling Effects of an Inhaled Highly Selective Phosphodiesterase 4 Inhibitor in Ventilated Preterm Lambs Exposed to Chorioamnionitis." Pharmaceuticals 16, no. 1 (2022): 29. http://dx.doi.org/10.3390/ph16010029.

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Phosphodiesterase (PDE) inhibition has been identified in animal studies as a new treatment option for neonatal lung injury, and as potentially beneficial for early lung development and function. However, our group could show that the inhaled PDE4 inhibitor GSK256066 could have dose-dependent detrimental effects and promote lung inflammation in the premature lung. In this study, the effects of a high and a low dose of GSK256066 on lung function, structure and alveolar development were investigated. In a triple hit lamb model of Ureaplasma-induced chorioamnionitis, prematurity, and mechanical v

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Han, Yongxin, André Giroux, Carole Lépine, et al. "Solid phase parallel synthesis of highly substituted thiophene derivatives and identification of novel phosphodiesterase-4 (PDE-4) inhibitors." Tetrahedron 55, no. 39 (1999): 11669–85. http://dx.doi.org/10.1016/s0040-4020(99)00686-9.

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Schwenkgrub, Joanna, Małgorzata Zaremba, Dagmara Mirowska-Guzel, and Iwona Kurkowska-Jastrzębska. "Ibudilast: a non-selective phosphodiesterase inhibitor in brain disorders." Postępy Higieny i Medycyny Doświadczalnej 71, no. 1 (2017): 0. http://dx.doi.org/10.5604/01.3001.0010.3798.

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Ibudilast (IBD) is a non-selective (3, 4, 10, 11) phosphodiesterase (PDE) inhibitor, used mainly as a bronchodilator for the treatment of bronchial asthma. PDE play a central role in cellular function (e.g. differentiation, synaptic plasticity and inflammatory response) by metabolizing cyclic nucleotides. The results from preclinical and clinical studies indicate that IBD has a broader range of action through suppression of pro-inflammatory cytokines (IL-6, IL-1β, TNF-α), toll-like receptor 4 blockade (TLR-4), inhibition of a macrophage migration inhibitory factor (MIF), up-regulation the anti

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Kolosionek, Ewa, Rajkumar Savai, Hossein Ardeschir Ghofrani, et al. "Expression and Activity of Phosphodiesterase Isoforms during Epithelial Mesenchymal Transition: The Role of Phosphodiesterase 4." Molecular Biology of the Cell 20, no. 22 (2009): 4751–65. http://dx.doi.org/10.1091/mbc.e09-01-0019.

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Epithelial–mesenchymal transition (EMT) has emerged as a critical event in the pathogenesis of organ fibrosis and cancer and is typically induced by the multifunctional cytokine transforming growth factor (TGF)-β1. The present study was undertaken to evaluate the potential role of phosphodiesterases (PDEs) in TGF-β1-induced EMT in the human alveolar epithelial type II cell line A549. Stimulation of A549 with TGF-β1 induced EMT by morphological alterations and by expression changes of the epithelial phenotype markers E-cadherin, cytokeratin-18, zona occludens-1, and the mesenchymal phenotype ma

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Lugnier, Claire. "The Complexity and Multiplicity of the Specific cAMP Phosphodiesterase Family: PDE4, Open New Adapted Therapeutic Approaches." International Journal of Molecular Sciences 23, no. 18 (2022): 10616. http://dx.doi.org/10.3390/ijms231810616.

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Cyclic nucleotides (cAMP, cGMP) play a major role in normal and pathologic signaling. Beyond receptors, cyclic nucleotide phosphodiesterases; (PDEs) rapidly convert the cyclic nucleotide in its respective 5′-nucleotide to control intracellular cAMP and/or cGMP levels to maintain a normal physiological state. However, in many pathologies, dysregulations of various PDEs (PDE1-PDE11) contribute mainly to organs and tissue failures related to uncontrolled phosphorylation cascade. Among these, PDE4 represents the greatest family, since it is constituted by 4 genes with multiple variants differently

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Boyd, Abigail, Ileana V. Aragon, Lina Abou Saleh, Dylan Southers та Wito Richter. "The cAMP-phosphodiesterase 4 (PDE4) controls β-adrenoceptor- and CFTR-dependent saliva secretion in mice". Biochemical Journal 478, № 10 (2021): 1891–906. http://dx.doi.org/10.1042/bcj20210212.

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Saliva, while often taken for granted, is indispensable for oral health and overall well-being, as inferred from the significant impairments suffered by patients with salivary gland dysfunction. Here, we show that treatment with several structurally distinct PAN-PDE4 inhibitors, but not a PDE3 inhibitor, induces saliva secretion in mice, indicating it is a class-effect of PDE4 inhibitors. In anesthetized mice, while neuronal regulations are suppressed, PDE4 inhibition potentiates a β-adrenoceptor-induced salivation, that is ablated by the β-blocker Propranolol and is absent from homozygous ΔF5

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Mazur, Małgorzata, Jacek Karczewski, Martha Lodyga, Ryszard Żaba, and Zygmunt Adamski. "Inhibitors of phosphodiesterase 4 (PDE 4): A new therapeutic option in the treatment of psoriasis vulgaris and psoriatic arthritis." Journal of Dermatological Treatment 26, no. 4 (2014): 326–28. http://dx.doi.org/10.3109/09546634.2014.991267.

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