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Journal articles on the topic 'PDE5 inhibitors'

Author: Grafiati

Published: 4 June 2021

Last updated: 1 February 2022

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1

Bloom, Timothy J. "Cyclic nucleotide phosphodiesterase isozymes expressed in mouse skeletal muscle." Canadian Journal of Physiology and Pharmacology 80, no. 12 (2002): 1132–35. http://dx.doi.org/10.1139/y02-149.

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To understand changes in cyclic nucleotide metabolism in muscle disease states, the expression of phosphodiesterase (PDE) isozymes in normal mouse leg muscle was examined. Four subcellular fractions were generated by differential centrifugation at 10 000 × g and 100 000 × g. cAMP PDE activity was found predominately in the soluble fractions, while cGMP PDE activity was more evenly distributed amongst soluble and particulate fractions. Pharmacological inhibitors demonstrate that PDE4 represents the major cAMP hydrolyzing activity and PDE2 represents the major cGMP hydrolyzing activity in mouse

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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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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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4

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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5

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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6

DAY, Jonathan P., Julian A. T. DOW, Miles D. HOUSLAY, and Shireen-A. DAVIES. "Cyclic nucleotide phosphodiesterases in Drosophila melanogaster." Biochemical Journal 388, no. 1 (2005): 333–42. http://dx.doi.org/10.1042/bj20050057.

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Cyclic nucleotide PDEs (phosphodiesterases) are important enzymes that regulate intracellular levels of cAMP and cGMP. In the present study, we identify and characterize novel PDEs in the genetic model, Drosophila melanogaster. The Drosophila genome encodes five novel PDE genes in addition to dunce. Predicted PDE sequences of Drosophila show highly conserved critical domains when compared with human PDEs. Thus PDE-encoding genes of D. melanogaster are CG14940-PDE1C, CG8279-PDE6β, CG5411-PDE8A, CG32648-PDE9 and CG10231-PDE11. Reverse transcriptase–PCRs of adult tissues reveal widespread express

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7

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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8

Wright, Lyndon C., Joachim Seybold, Annette Robichaud, Ian M. Adcock, and Peter J. Barnes. "Phosphodiesterase expression in human epithelial cells." American Journal of Physiology-Lung Cellular and Molecular Physiology 275, no. 4 (1998): L694—L700. http://dx.doi.org/10.1152/ajplung.1998.275.4.l694.

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Epithelial cells play a critical role in airway inflammation and have the capacity to produce many inflammatory mediators, including bioactive lipids and proinflammatory cytokines. Intracellular levels of cAMP and cGMP are important in the control of inflammatory cell function. These cyclic nucleotides are inactivated via a family of phosphodiesterase (PDE) enzymes, providing a possible site for drug intervention in chronic inflammatory conditions. We studied the expression of PDE activity in an epithelial cell line (A549) and in primary human airway epithelial cells (HAECs). We measured PDE f

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9

Hussein, Abdel Haleem M., Ahmed A. Khames, Abu-Bakr A. El-Adasy, et al. "Multifunctional Isosteric Pyridine Analogs-Based 2-Aminothiazole: Design, Synthesis, and Potential Phosphodiesterase-5 Inhibitory Activity." Molecules 26, no. 4 (2021): 902. http://dx.doi.org/10.3390/molecules26040902.

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The elaboration of new small molecules that target phosphodiesterase enzymes (PDEs), especially those of type 5 (PDE5), is an interesting and emerging topic nowadays. A new series of heterocycle-based aminothiazoles were designed and synthesized from the key intermediate, 3-oxo-N-(thiazol-2-yl)butanamide (a PDE5 inhibitor that retains its amidic function), as an essential pharmacophoric moiety. The PDE5 inhibitors prevent the degradation of cyclic guanosine monophosphate, thereby causing severe hypotension as a marked side effect. Hence, an in vivo testing of the target compounds was conducted

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Tulsian, Nikhil K., Valerie Jia-En Sin, Hwee-Ling Koh, and Ganesh S. Anand. "Development of Phosphodiesterase–Protein-Kinase Complexes as Novel Targets for Discovery of Inhibitors with Enhanced Specificity." International Journal of Molecular Sciences 22, no. 10 (2021): 5242. http://dx.doi.org/10.3390/ijms22105242.

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Phosphodiesterases (PDEs) hydrolyze cyclic nucleotides to modulate multiple signaling events in cells. PDEs are recognized to actively associate with cyclic nucleotide receptors (protein kinases, PKs) in larger macromolecular assemblies referred to as signalosomes. Complexation of PDEs with PKs generates an expanded active site that enhances PDE activity. This facilitates signalosome-associated PDEs to preferentially catalyze active hydrolysis of cyclic nucleotides bound to PKs and aid in signal termination. PDEs are important drug targets, and current strategies for inhibitor discovery are ba

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11

Zenzmaier, Christoph, Natalie Sampson, Dominik Pernkopf, Eugen Plas, Gerold Untergasser, and Peter Berger. "Attenuated Proliferation and Trans-Differentiation of Prostatic Stromal Cells Indicate Suitability of Phosphodiesterase Type 5 Inhibitors for Prevention and Treatment of Benign Prostatic Hyperplasia." Endocrinology 151, no. 8 (2010): 3975–84. http://dx.doi.org/10.1210/en.2009-1411.

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Benign prostatic hyperplasia (BPH) is characterized by tissue overgrowth and stromal reorganization primarily due to cellular proliferation and fibroblast-to-myofibroblast trans-differentiation. To evaluate the potential of phosphodiesterase type 5 (PDE5) inhibitors like tadalafil for prevention and treatment of BPH, we analyzed the role of the nitric oxide/cyclic GMP (cGMP)/PDE5 pathway for cellular proliferation and TGFβ1-induced fibroblast-to-myofibroblast trans-differentiation in primary prostate stromal cells. Inhibition by tadalafil of PDE5, which is mainly expressed in the stromal compa

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Azizi, Aziemah, Asrin Tengah, and Mark I. R. Petalcorin. "Developing a phosphodiesterase-5 inhibitor assay to detect counterfeit drugs containing phosphodiesterase-5 inhibitors using spectrophotometry." F1000Research 8 (September 26, 2019): 1692. http://dx.doi.org/10.12688/f1000research.19500.1.

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Background: Phosphodiesterase-5 inhibitors (PDE5i) are the first line of drugs used for the treatment of erectile dysfunction. PDE5i inhibits the activities of phosphodiesterase-5 (PDE5) found in corpus cavernosum reducing production of guanosine monophosphate (GMP) that results in vasodilation of blood vessels thereby prolonging penile erection. Various counterfeit drugs adulterated with unknown levels of PDE5i pose a danger with reported undesirable adverse effects on patients. Methods: We developed an assay to detect counterfeit drugs containing PDE5i using spectrophotometry based on a colo

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13

Mouli, S., and K. T. McVary. "PDE5 inhibitors for LUTS." Prostate Cancer and Prostatic Diseases 12, no. 4 (2009): 316–24. http://dx.doi.org/10.1038/pcan.2009.27.

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14

Nardozza Junior, Archimedes, and Marcelo Rodrigues Cabrini. "Daily use of phosphodiesterase type 5 inhibitors as prevention for recurrent priapism." Revista da Associação Médica Brasileira 63, no. 8 (2017): 689–92. http://dx.doi.org/10.1590/1806-9282.63.08.689.

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Summary Objective: The pathogenesis of recurrent priapism is currently being investigated based on the regulation of the phosphodiesterase 5 (PDE5) enzyme. We explored the daily use of PDE5 inhibitors to treat and prevent priapism recurrences. Method: We administered PDE5 inhibitors using a long-term therapeutic regimen in seven men with recurrent priapism, with a mean age of 29.2 years (range 21 to 35 years). Six men (85.7%) had idiopathic priapism recurrences and one man (24.3%) had sickle cell disease-associated priapism recurrences. Tadalafil 5 mg was administered daily. The mean follow-up

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15

Sharvadze, G. G., R. R. Dalari, B. U. Mardanov, and M. N. Mamedov. "MANAGEMENT OF ERECTILE DYSFUNCTION IN CARDIOVASCULAR PATIENTS WITH COMORBIDITIES: REVIEW OF THE TRIALS ON CONTINUING THERAPY WITH PHOSPHODIESTERASE-5 MEDICATIONS." Cardiovascular Therapy and Prevention 17, no. 3 (2018): 79–84. http://dx.doi.org/10.15829/1728-8800-2018-3-79-84.

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The review is focused on the issues of erectile dysfunction (ED) management by long term courses of continuous intake of the phosphodiesteraze-5 type (PDE5) inhibitors. ED is an actual problem of modern healthcare, prevalent and influencing negatively life quality and interpersonal relations. At early stages the management of ED by the PDE5 inhibitor drugs was regarded as symptomatic. However recently there are more and more publications that confirm continuous long term intake of PDE5 inhibitors. This can be explained by the mechanism of this drugs class action that includes the causation of

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16

Hutchings, David Charles, Simon George Anderson, Jessica L. Caldwell, and Andrew W. Trafford. "Phosphodiesterase-5 inhibitors and the heart: compound cardioprotection?" Heart 104, no. 15 (2018): 1244–50. http://dx.doi.org/10.1136/heartjnl-2017-312865.

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Novel cardioprotective agents are needed in both heart failure (HF) and myocardial infarction. Increasing evidence from cellular studies and animal models indicate protective effects of phosphodiesterase-5 (PDE5) inhibitors, drugs usually reserved as treatments of erectile dysfunction and pulmonary arterial hypertension. PDE5 inhibitors have been shown to improve contractile function in systolic HF, regress left ventricular hypertrophy, reduce myocardial infarct size and suppress ischaemia-induced ventricular arrhythmias. Underpinning these actions are complex but increasingly understood cellu

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17

Setter, Stephen M., Jason L. Iltz, Jack E. Fincham, R. Keith Campbell, and Danial E. Baker. "Phosphodiesterase 5 Inhibitors for Erectile Dysfunction." Annals of Pharmacotherapy 39, no. 7-8 (2005): 1286–95. http://dx.doi.org/10.1345/aph.1e487.

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OBJECTIVE To review the pharmacologic and clinical trial data of the Food and Drug Administration–approved phosphodiesterase 5 (PDE5) inhibitors for the treatment of erectile dysfunction (ED). DATA SOURCES Primary research and review articles were identified through a search of ScienceDirect, PubMed/MEDLINE, and International Pharmaceutical Abstracts (1990–August 2004). The following search terms were used in the Medicine Dentistry and Pharmacology, Toxicology, and Pharmaceutical Sciences subcategories: phosphodiesterase 5 inhibitor, PDE5 inhibitor, erectile dysfunction, sildenafil, vardenafil

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18

Boyle, Craig D., Ruo Xu, Theodros Asberom, et al. "Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED." Bioorganic & Medicinal Chemistry Letters 15, no. 9 (2005): 2365–69. http://dx.doi.org/10.1016/j.bmcl.2005.02.083.

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19

Giovannoni, M. P., C. Vergelli, A. Graziano, and V. Dal Piaz. "PDE5 Inhibitors and their Applications." Current Medicinal Chemistry 999, no. 999 (2010): 1–24. http://dx.doi.org/10.2174/0929210204916348673.

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20

Giovannoni, M. P., C. Vergelli, A. Graziano, and V. Dal Piaz. "PDE5 Inhibitors and their Applications." Current Medicinal Chemistry 17, no. 24 (2010): 2564–87. http://dx.doi.org/10.2174/092986710791859360.

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21

Sandner, P., J. Hütter, H. Tinel, K. Ziegelbauer, and E. Bischoff. "PDE5 inhibitors beyond erectile dysfunction." International Journal of Impotence Research 19, no. 6 (2007): 533–43. http://dx.doi.org/10.1038/sj.ijir.3901577.

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22

Hackett, G. I. "Further reassurance regarding PDE5 inhibitors." International Journal of Clinical Practice 61, no. 9 (2007): 1426–27. http://dx.doi.org/10.1111/j.1742-1241.2007.01486.x.

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23

Taylor, Justin S. W., and Julian P. J. Halcox. "PDE5 inhibitors and pulmonary hypertension." Current Sexual Health Reports 5, no. 4 (2008): 171–78. http://dx.doi.org/10.1007/s11930-008-0031-8.

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24

Kimura, Hiroshi, and Kaoru Hamada. "2. Phosphodiesterase-5 Inhibitors." Nihon Naika Gakkai Zasshi 99, no. 7 (2010): 1557–62. http://dx.doi.org/10.2169/naika.99.1557.

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Mokra, Daniela, and Juraj Mokry. "Phosphodiesterase Inhibitors in Acute Lung Injury: What Are the Perspectives?" International Journal of Molecular Sciences 22, no. 4 (2021): 1929. http://dx.doi.org/10.3390/ijms22041929.

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Despite progress in understanding the pathophysiology of acute lung damage, currently approved treatment possibilities are limited to lung-protective ventilation, prone positioning, and supportive interventions. Various pharmacological approaches have also been tested, with neuromuscular blockers and corticosteroids considered as the most promising. However, inhibitors of phosphodiesterases (PDEs) also exert a broad spectrum of favorable effects potentially beneficial in acute lung damage. This article reviews pharmacological action and therapeutical potential of nonselective and selective PDE

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26

Cai, Ying-Lan, Mo-Han Zhang, Xu Huang, et al. "CNP-pGC-cGMP-PDE3-cAMP Signal Pathway Upregulated in Gastric Smooth Muscle of Diabetic Rats." Gastroenterology Research and Practice 2015 (2015): 1–9. http://dx.doi.org/10.1155/2015/305258.

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Our previous studies have shown that CNP-NPR-B/pGC-cGMP is upregulated in the diabetic rats. The present study was designed to determine whether the upregulation of CNP-NPR-B/pGC-cGMP signal pathway affects cGMP-PDE3-cAMP signal pathway in diabetic gastric smooth muscle. The gastric smooth muscle motility was observed by using isometric measurement. PDEs expressions in diabetic gastric smooth muscle tissue were observed by using immunohistochemistry, Western blotting, and RT-PCR methods. The results demonstrated that the inhibitory effect of CNP on the spontaneous contraction of gastric antral

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Yakovleva, O. A., A. I. Semenenko, and O. Yu Hoina-Kardasevich. "New targets of pharmacotherapy of bronchial obstruction." Infusion & Chemotherapy, no. 3.1 (October 11, 2020): 87–88. http://dx.doi.org/10.32902/2663-0338-2020-3.1-73.

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Objective. To assess the prospects for scientific development of new classes of bronchodilators for respiratory diseases with obstructive syndrome, taking into account future molecular targets. Materials and methods. The analysis of international English scientific information in the systems of surveys and search on the Internet for the last 5 years is carried out. Results and discussion. Currently, there is an increasing interest in the development of new directions for pharmacological correction of the mechanisms of bronchial obstruction. The proposed international protocols are

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28

Russo, I., P. Del Mese, G. Doronzo, et al. "Resistance to the Nitric Oxide/Cyclic Guanosine 5′-Monophosphate/Protein Kinase G Pathway in Vascular Smooth Muscle Cells from the Obese Zucker Rat, a Classical Animal Model of Insulin Resistance: Role of Oxidative Stress." Endocrinology 149, no. 4 (2007): 1480–89. http://dx.doi.org/10.1210/en.2007-0920.

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Some in vivo and ex vivo studies demonstrated a resistance to the vasodilating effects of nitric oxide (NO) in insulin-resistant states and, in particular, obese Zucker rats (OZR). To evaluate the biochemical basis of this phenomenon, we aimed to identify defects of the NO/cGMP/cGMP-dependent protein kinase (PKG) pathway in cultured vascular smooth muscle cells (VSMCs) from OZR and lean Zucker rats (LZR) by measuring: 1) NO donor ability to increase cGMP in the absence and presence of inhibitors of soluble guanylate cyclase (sGC) and phosphodiesterases (PDEs); 2) NO and cGMP ability to induce,

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29

Santos, Ana I., Bruno P. Carreira, Rui J. Nobre, Caetana M. Carvalho, and Inês M. Araújo. "Stimulation of Neural Stem Cell Proliferation by Inhibition of Phosphodiesterase 5." Stem Cells International 2014 (2014): 1–13. http://dx.doi.org/10.1155/2014/878397.

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The involvement of nitric oxide (NO) and cyclic GMP (cGMP) in neurogenesis has been progressively unmasked over the last decade. Phosphodiesterase 5 (PDE5) specifically degrades cGMP and is highly abundant in the mammalian brain. Inhibition of cGMP hydrolysis by blocking PDE5 is a possible strategy to enhance the first step of neurogenesis, proliferation of neural stem cells (NSC). In this work, we have studied the effect on cell proliferation of 3 inhibitors with different selectivity and potency for PDE5, T0156, sildenafil, and zaprinast, using subventricular zone-(SVZ-) derived NSC cultures

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30

Kniotek, Monika, and Agnieszka Boguska. "Sildenafil Can Affect Innate and Adaptive Immune System in Both Experimental Animals and Patients." Journal of Immunology Research 2017 (2017): 1–8. http://dx.doi.org/10.1155/2017/4541958.

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Sildenafil, a type 5 phosphodiesterase inhibitor (PDE5-I), is primarily used for treating erectile dysfunction. Sildenafil inhibits the degradation of cyclic guanosine monophosphate (cGMP) by competing with cGMP for binding site of PDE5. cGMP is a secondary messenger activating protein kinases and a common regulator of ion channel conductance, glycogenolysis, and cellular apoptosis. PDE5 inhibitors (PDE-Is) found application in cardiology, nephrology, urology, dermatology, oncology, and gynecology. Positive result of sildenafil treatment is closely connected with its immunomodulatory effects.

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Sybertz, Edmund, and Michael Czarniecki. "Inhibitors of PDE1 and PDE5 cGMP phosphodiesterases: patents and therapeutic potential." Expert Opinion on Therapeutic Patents 7, no. 6 (1997): 631–39. http://dx.doi.org/10.1517/13543776.7.6.631.

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32

Rybalkin, Sergei, and Karin Bornfeldt. "Cyclic Nucleotide Phosphodiesterases and Human Arterial Smooth Muscle Cell Proliferation." Thrombosis and Haemostasis 82, no. 08 (1999): 424–34. http://dx.doi.org/10.1055/s-0037-1615862.

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IntroductionSmooth muscle cells (SMCs) in the arterial wall are normally found in a contractile, nonproliferative state. These SMCs are continuously exposed to agents that elevate cyclic AMP (cAMP) and cyclic GMP (cGMP), such as prostacyclin and nitric oxide (NO) released from the endothelium. Both cAMP and cGMP potently inhibit SMC proliferation by antagonizing major signaling pathways induced by growth factors, such as platelet-derived growth factor. Different forms of injury to the endothelium result in proliferation of the SMCs and can develop into atherosclerosis, restenosis, or arterial

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Sharlip, Ira D. "PDE5 Inhibitors Do Not Cause NAION." Journal of Sexual Medicine 3 (March 2006): 80. http://dx.doi.org/10.1111/j.1743-6109.2006.00190.x.

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Tomsak, R. "PDE5 inhibitors and permanent visual loss." International Journal of Impotence Research 17, no. 6 (2005): 547–49. http://dx.doi.org/10.1038/sj.ijir.3901396.

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HACKETT, G. "PDE5 inhibitors in diabetic peripheral neuropathy." International Journal of Clinical Practice 60, no. 9 (2006): 1123–26. http://dx.doi.org/10.1111/j.1742-1241.2006.01087.x.

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Vlachopoulos, C., D. Terentes-Printzios, N. Ioakeimidis, K. Rokkas, and C. Stefanadis. "PDE5 Inhibitors in Non-Urological Conditions." Current Pharmaceutical Design 15, no. 30 (2009): 3521–39. http://dx.doi.org/10.2174/138161209789206980.

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37

Clyne, Melanie. "Can PDE5 inhibitors boost brain function?" Nature Reviews Urology 11, no. 2 (2013): 65. http://dx.doi.org/10.1038/nrurol.2013.309.

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Abusnina, Abdurazzag, Thérèse Keravis, Qingwei Zhou, Hélène Justiniano, Annelise Lobstein, and Claire Lugnier. "Tumour growth inhibition and anti-angiogenic effects using curcumin correspond to combined PDE2 and PDE4 inhibition." Thrombosis and Haemostasis 113, no. 02 (2015): 319–28. http://dx.doi.org/10.1160/th14-05-0454.

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SummaryVascular endothelial growth factor (VEGF) plays a major role in angiogenesis by stimulating endothelial cells. Increase in cyclic AMP (cAMP) level inhibits VEGF-induced endothelial cell proliferation and migration. Cyclic nucleotide phosphodiesterases (PDEs), which specifically hydrolyse cyclic nucleotides, are critical in the regulation of this signal transduction. We have previously reported that PDE2 and PDE4 up-regulations in human umbilical vein endothelial cells (HUVECs) are implicated in VEGF-induced angiogenesis and that inhibition of PDE2 and PDE4 activities prevents the develo

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Vaclavik, Lukas, John R. Schmitz, Jean-Francois Halbardier, and Katerina Mastovska. "Single-Laboratory Validation Study of a Method for Screening and Identification of Phosphodiesterase Type 5 Inhibitors in Dietary Ingredients and Supplements Using Liquid Chromatography/Quadrupole–Orbital Ion Trap Mass Spectrometry: First Action 2015.12." Journal of AOAC INTERNATIONAL 99, no. 1 (2016): 55–72. http://dx.doi.org/10.5740/jaoacint.15-0202.

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Abstract A single-laboratory validation study of a method for screening and identification of phosphodiesterase type 5 (PDE5) inhibitors in dietary ingredients and supplements is described. PDE5 inhibitors were extracted from the samples using a 50:50 (v/v) mixture of acetonitrile and water and centrifuged. Supernatant was diluted, filtered, and analyzed by LC–high-resolution MS. Data were collected in MS acquisition mode that combined full-scan MS experiment with all-ion fragmentation and data-dependent MS/MS product from the ion scan experiment. This approach enabled collection of MS and tan

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Kodchakorn, Kanchanok, Nawarat Viriyakhasem, Tunchanok Wongwichai, and Prachya Kongtawelert. "Structural Determination, Biological Function, and Molecular Modelling Studies of Sulfoaildenafil Adulterated in Herbal Dietary Supplement." Molecules 26, no. 4 (2021): 949. http://dx.doi.org/10.3390/molecules26040949.

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Unapproved ingredients included in herbal medicines and dietary supplements have been detected as adulterated synthetic drugs used for erectile dysfunction. Extraction from a dietary supplement was performed to isolate the compounds by HPLC analysis. The structural characterization was confirmed using mass spectrometry (ESI-TOF/MS and LC-MS/MS), 1H NMR, and 13C NMR spectroscopy techniques. Results identified the thus-obtained compound to be sulfoaildenafil, a thioketone analogue of sildenafil. The biological activities of this active compound have been focused for the first time by the experim

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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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Wang, Huanchen, Stefan Kunz, Gong Chen, et al. "Biological and Structural Characterization of Trypanosoma cruzi Phosphodiesterase C and Implications for Design of Parasite Selective Inhibitors." Journal of Biological Chemistry 287, no. 15 (2012): 11788–97. http://dx.doi.org/10.1074/jbc.m111.326777.

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Trypanosoma cruzi phosphodiesterase C (TcrPDEC) is a potential new drug target for the treatment of Chagas disease but has not been well studied. This study reports the enzymatic properties of various kinetoplastid PDECs and the crystal structures of the unliganded TcrPDEC1 catalytic domain and its complex with an inhibitor. Mutations of PDEC during the course of evolution led to inactivation of PDEC in Trypanosoma brucei/Trypanosoma evansi/Trypanosoma congolense, whereas the enzyme is active in all other kinetoplastids. The TcrPDEC1 catalytic domain hydrolyzes both cAMP and cGMP with a Km of

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Zhu, Bing, Li Zhang, Mikhail Alexeyev, Diego F. Alvarez, Samuel J. Strada, and Troy Stevens. "Type 5 phosphodiesterase expression is a critical determinant of the endothelial cell angiogenic phenotype." American Journal of Physiology-Lung Cellular and Molecular Physiology 296, no. 2 (2009): L220—L228. http://dx.doi.org/10.1152/ajplung.90474.2008.

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Type 5 phosphodiesterase (PDE5) inhibitors increase endothelial cell cGMP and promote angiogenesis. However, not all endothelial cell phenotypes express PDE5. Indeed, whereas conduit endothelial cells express PDE5, microvascular endothelial cells do not express this enzyme, and they are rapidly angiogenic. These findings bring into question whether PDE5 activity is a critical determinant of the endothelial cell angiogenic potential. To address this question, human full-length PDE5A1 was stably expressed in pulmonary microvascular endothelial cells. hPDE5A1 expression reduced the basal and atri

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de Oliveira, Ivan Pires, Caroline Honaiser Lescano, and Gilberto De Nucci. "In Silico Mapping of Essential Residues in the Catalytic Domain of PDE5 Responsible for Stabilization of Its Commercial Inhibitors." Scientia Pharmaceutica 87, no. 4 (2019): 29. http://dx.doi.org/10.3390/scipharm87040029.

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Phosphodiesterase type 5 (PDE5) is an important enzyme associated with the hydrolysis of cyclic guanosine monophosphate (cGMP) to guanosine monophosphate (GMP). Due to the relevant role of second messenger cGMP as a mediator in many physiological processes, efforts have been converged to find a safe pharmacological approach, seeking a specific, selective and potent inhibitor of the PDE5 enzyme. There are five commercial drugs with potential for clinical use: tadalafil, sildenafil, avanafil, udenafil and vardenafil. Here, we applied molecular modeling to obtain different profiles of protein–lig

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Zenzmaier, Christoph, Johann Kern, Natalie Sampson, et al. "Phosphodiesterase Type 5 Inhibition Reverts Prostate Fibroblast-to-Myofibroblast Trans-Differentiation." Endocrinology 153, no. 11 (2012): 5546–55. http://dx.doi.org/10.1210/en.2012-1431.

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Abstract Phosphodiesterase type 5 (PDE5) inhibitors have been demonstrated to improve lower urinary tract symptoms secondary to benign prostatic hyperplasia (BPH). Because BPH is primarily driven by fibroblast-to-myofibroblast trans-differentiation, this study aimed to evaluate the potential of the PDE5 inhibitor vardenafil to inhibit and reverse trans-differentation of primary human prostatic stromal cells (PrSC). Vardenafil, sodium nitroprusside, lentiviral-delivered short hairpin RNA-mediated PDE5 knockdown, sodium orthovanadate, and inhibitors of MAPK kinase, protein kinase G, Ras homolog

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Vignozzi, Linda, Mauro Gacci, Ilaria Cellai, et al. "PDE5 inhibitors blunt inflammation in human BPH: A potential mechanism of action for PDE5 inhibitors in LUTS." Prostate 73, no. 13 (2013): 1391–402. http://dx.doi.org/10.1002/pros.22686.

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MURTHY, Karnam S. "Activation of phosphodiesterase 5 and inhibition of guanylate cyclase by cGMP-dependent protein kinase in smooth muscle." Biochemical Journal 360, no. 1 (2001): 199–208. http://dx.doi.org/10.1042/bj3600199.

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The regulation of cGMP-specific phosphodiesterase (PDE) 5 and soluble guanylate cyclase (GC) by cGMP- and cAMP-dependent protein kinases (PKG and PKA respectively) was examined in gastric smooth muscle. The NO donor, sodium nitroprusside (SNP), stimulated PDE5 phosphorylation and activity, which was blocked by the selective PKG inhibitor, KT5823, resulting in an elevation of cGMP levels. Activation of PKA either directly by Sp-5,6-dichloro-1-β-d-ribofuranosyl benzimidazole 3′,5′-cyclic monophosphothioate, or via isoproterenol- and forskolin-dependent increase in cAMP, also caused an increase i

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Barbagallo, Federica, Federica Campolo, Edoardo Franceschini, et al. "PDE5 Inhibitors in Type 2 Diabetes Cardiovascular Complications." Endocrines 1, no. 2 (2020): 90–101. http://dx.doi.org/10.3390/endocrines1020009.

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Pharmacological inhibition of Phosphodiesterase type 5 (PDE5) proved its efficacy treating several pathological conditions, such as erectile dysfunction and pulmonary hypertension. Nowadays, its benefits on cardiovascular diseases are well documented, particularly in the treatment of type 2 diabetes (T2DM)-related cardiovascular complications. In this context, treatment of T2DM with PDE5 inhibitors, such as sildenafil, tadalafil or vardenafil ameliorates endothelial dysfunction both in patients and animal models through an augmented flow mediated dilation rate and an up-regulation of endotheli

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Hisasue, Shin-ichi. "The future of Men’s health with PDE5-inhibitors." Folia Pharmacologica Japonica 147, no. 1 (2016): 45–47. http://dx.doi.org/10.1254/fpj.147.45.

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Bowles, Elizabeth, Randy Sprague, and Nuran Ercal. "Liposomal Delivery of a Phosphodiesterase 5 Inhibitor Enhances Prostacyclin-Mediated Adenosine Triphosphate Release from Human Red Blood Cells." Blood 128, no. 22 (2016): 4803. http://dx.doi.org/10.1182/blood.v128.22.4803.4803.

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Abstract Pulmonary arterial hypertension (PAH) is characterized by high pulmonary vascular resistance (PVR) and right heart failure. Red blood cells (RBCs) of PAH patients fail to release the vasodilator, adenosine triphosphate (ATP), when deformed as would occur when traversing the lung. Such a defect could contribute to increased PVR. However, RBCs of PAH patients do release ATP in response to prostacyclin (PGI2) analogs and this is augmented by phosphodiesterase 5 (PDE5) inhibitors. Current PAH treatment includes PGI2 analogs and PDE5 inhibitors alone or in combination. Unfortunately, these

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