Genomes and Genes
Gene Symbol: PDE5A
Description: phosphodiesterase 5A
Alias: CGB-PDE, CN5A, PDE5, cGMP-specific 3',5'-cyclic phosphodiesterase, cGMP-binding cGMP-specific 3',5'-cyclic nucleotide phosphodiesterase, cGMP-specific phosphodiesterase PDE5A2, cGMP-specific phosphodiesterase type 5A, phosphodiesterase 5A, cGMP-specific, phosphodiesterase isozyme 5
Publications264 found, 100 shown here
- Substrate- and kinase-directed regulation of phosphorylation of a cGMP-binding phosphodiesterase by cGMPM K Thomas
Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 0615
J Biol Chem 265:14971-8. 1990..Such regulation would greatly increase the selectivity of the phosphorylation of cG-BPDE and would represent a unique mechanism of action of a cyclic nucleotide or other second messenger...
- PDE5 is converted to an activated state upon cGMP binding to the GAF A domainSergei D Rybalkin
Department of Pharmacology, University of Washington, Seattle, WA 98195 7280, USA
EMBO J 22:469-78. 2003cGMP-specific, cGMP-binding phosphodiesterase (PDE5) regulates such physiological processes as smooth muscle relaxation and neuronal survival...
- Ventricular phosphodiesterase-5 expression is increased in patients with advanced heart failure and contributes to adverse ventricular remodeling after myocardial infarction in micePeter Pokreisz
Vesalius Research Center, Flanders Institute for Biotechnology, Leuven, Belgium
Circulation 119:408-16. 2009Ventricular expression of phosphodiesterase-5 (PDE5), an enzyme responsible for cGMP catabolism, is increased in human right ventricular hypertrophy, but its role in left ventricular (LV) failure remains incompletely understood...
- Oxidative stress regulates left ventricular PDE5 expression in the failing heartZhongbing Lu
Cardiovascular Division, University of Minnesota, Minneapolis, MN 55455, USA
Circulation 121:1474-83. 2010Phosphodiesterase type 5 (PDE5) inhibition has been shown to exert profound beneficial effects in the failing heart, suggesting a significant role for PDE5 in the development of congestive heart failure (CHF)...
- Direct activation of PDE5 by cGMP: long-term effects within NO/cGMP signalingFlorian Mullershausen
Abteilung für Pharmakologie und Toxikologie, Medizinische Fakultat, Ruhr Universitat Bochum, MA N1 43, Universitaetsstr 150, 44780 Bochum, Germany
J Cell Biol 160:719-27. 2003..within the NO-induced cGMP response in human platelets, activation and phosphorylation of phosphodiesterase type 5 (PDE5) occurred...
- Cyclic AMP-specific and cyclic GMP-specific phosphodiesterase isoenzymes in human cavernous arteries--immunohistochemical distribution and functional significanceEginhard Waldkirch
Department of Urology, Hannover Medical School, 30625, Hannover, Germany
World J Urol 23:405-10. 2005....
- PDE4 and PDE5 regulate cyclic nucleotides relaxing effects in human umbilical arteriesAntónio José Santos-Silva
Centro de Investigacao em Ciencias da Saude, Universidade da Beira Interior, Av Infante D Henrique, 6200 506 Covilha, Portugal
Eur J Pharmacol 582:102-9. 2008..umbilical artery smooth muscle was analysed by RT-PCR and the expression of PDE1B, PDE3A, PDE3B, PDE4C, PDE4D and PDE5A was detected...
- Antenatal sildenafil treatment attenuates pulmonary hypertension in experimental congenital diaphragmatic herniaChristina Luong
Department of Pediatrics, Women and Children Health Research Institute, Cardiovascular Research Group, University of Alberta, Edmonton, Canada
Circulation 123:2120-31. 2011..Phosphodiesterase type 5 (PDE5) limits the effects of NO by inactivation of cyclic GMP...
- Role of a novel tetrodotoxin-resistant sodium channel in the nitrergic relaxation of corpus cavernosum from the South American rattlesnake Crotalus durissus terrificusRodrigo O Capel
Department of Pharmacology, Faculty of Medical Sciences, State University of Campinas UNICAMP, Campinas, SP, Brazil
J Sex Med 8:1616-25. 2011..Coitus in snakes may last up to 28 hours; however, the mechanisms involved are unknown...
- Expression of messenger ribonucleic acid encoding for phosphodiesterase isoenzymes in human female genital tissuesStefan Uckert
Hannover Medical School Department of Urology, Hannover, Germany, and IPF Pharmaceuticals GmbH Urological Research Unit, Hannover, Germany
J Sex Med 4:1604-9. 2007The use of inhibitors of phosphodiesterase 5 (PDE5) has been suggested to treat symptoms of female sexual dysfunction (FSD)...
- Effects of phosphodiesterase inhibitors on tension induced by norepinephrine and accumulation of cyclic nucleotides in isolated human prostatic tissueStefan Uckert
Department of Urology, Hannover Medical School, Hannover, Germany
Urology 71:526-30. 2008..the mechanism of action of phosphodiesterase (PDE) inhibitors on the human prostate, the effects of PDE4 and PDE5 inhibitors on the tension induced by norepinephrine (NE) and on the intracellular levels of cyclic nucleotides in ..
- Phosphodiesterase 3 and 5 and cyclic nucleotide-gated ion channel expression in rat trigeminovascular systemLars S Kruse
Department of Neurology, Glostrup Hospital, Nordre Ringvej 57, Denmark
Neurosci Lett 404:202-7. 2006..For comparison, rat aorta and mesenteric artery were analysed. PDE3A, PDE3B, and PDE5A mRNA were detected in all tissues examined except for PDE3A mRNA in dura mater and the trigeminal ganglion...
- Experimental studies on guanosine 3',5'-cyclic monophosphate levels and airway responsiveness of the novel phosphodiesterase type 5 inhibitor SR 265579 in guinea-pigsZ Kapui
Biological Research Department, Chinoin Pharmaceutical and Chemicals Works, Budapest, Hungary
Arzneimittelforschung 49:685-93. 1999..SR 265579), a potent inhibitor of guanosine 3',5'-cyclic monophosphate (cyclic GMP) phosphodiesterase (PDE5), was examined regarding its specificity toward the other cyclic nucleotide phosphodiesterases, the effect on ..
- Effects of phosphodiesterase inhibitors on the contractile responses of isolated human seminal vesicle tissue to adrenergic stimulationStefan Uckert
Division of Surgery, Department of Urology, Hannover Medical School, Hannover, Germany
J Sex Med 6:408-14. 2009It has been suggested that the capability of the phosphodiesterase 5 (PDE5) inhibitor sildenafil citrate (VIAGRA) to retard the ejaculatory response may include modulation of the contraction of seminal vesicle (SV) smooth muscle...
- Phosphodiesterase inhibitors and the eyeNathan M Kerr
Department of Ophthalmology, Faculty of Medical and Health Sciences, University of Auckland, Auckland, New Zealand
Clin Experiment Ophthalmol 37:514-23. 2009Phosphodiesterase type 5 (PDE5) inhibitors are effective oral treatments for erectile dysfunction and have become one of the most widely prescribed medications worldwide...
- Pharmacology and drug interaction effects of the phosphodiesterase 5 inhibitors: focus on alpha-blocker interactionsRobert A Kloner
Heart Institute, Good Samaritan Hospital, Keck School of Medicine, University of Southern California, Los Angeles, CA 90017, USA
Am J Cardiol 96:42M-46M. 2005Currently, 3 phosphodiesterase 5 (PDE5) inhibitor agents are available worldwide for the treatment of erectile dysfunction (ED): sildenafil, vardenafil, and tadalafil...
- Effect of sildenafil on middle-aged sexually active males with no erectile complaints: a randomized placebo-controlled double-blind studyIlan Gruenwald
Neuro urology unit, Rambam Health Care Campus and the Technion Faculty of Medicine, Haifa, Israel
Eur Urol 55:969-76. 2009In clinical practice, we commonly encounter sexually healthy males who use phosphodiesterase type 5 (PDE5) inhibitors and report a beneficial effect to their sex life.
- Combination of doxazosin and sildenafil exerts an additive relaxing effect compared with each compound alone on human cavernosal and prostatic tissueStephanie Oger
Pelvipharm, Orsay Parc, Orsay, France
J Sex Med 6:836-47. 2009Phosphodiesterase 5 inhibitors (PDE5) such as sildenafil are first-line treatment for erectile dysfunction (ED)...
- Phosphodiesterase type 5 regulation in the penile corpora cavernosaChing Shwun Lin
Knuppe Molecular Urology Laboratory, University of California, Department of Urology, San Francisco, CA 94115, USA
J Sex Med 6:203-9. 2009Penile detumescence depends on the hydrolysis of cyclic guanosine monophosphate (cGMP) by phosphodiesterase type 5 (PDE5)...
- Concerted regulation of cGMP and cAMP phosphodiesterases in early cardiac hypertrophy induced by angiotensin IIWalid Mokni
CNRS UMR 7213, Biophotonique et Pharmacologie, Faculte de Pharmacie, Universite de Strasbourg, Illkirch, France
PLoS ONE 5:e14227. 2010..130% for PDE1; +76% for PDE2; +113% for PDE5) and associated with increased expressions for PDE1A, PDE1C and PDE5A. The cGMP-PDE1 activation by Ca(2+)/CaM was reduced. BNP expression was increased by 3...
- PDE5A inhibition attenuates bleomycin-induced pulmonary fibrosis and pulmonary hypertension through inhibition of ROS generation and RhoA/Rho kinase activationAnna R Hemnes
Division of Cardiology, Department of Medicine, Johns Hopkins University School of Medicine, 720 Rutland Ave, Ross 850, Baltimore, MD 21205, USA
Am J Physiol Lung Cell Mol Physiol 294:L24-33. 2008..lung disease-associated pulmonary hypertension, and this process can be abrogated by phosphodiesterase type 5 (PDE5) inhibition to improve pulmonary vascular remodeling and right ventricular function...
- Effectiveness of sildenafil citrate (Viagra) and tadalafil (Cialis) on sexual responses in Saudi men with erectile dysfunction in routine clinical practiceSyed Tabrez Ali
Department of Physiology, Faculty of Medicine, Umm Al Qura University, Makkah, Saudi Arabia
Pak J Pharm Sci 21:275-81. 2008..Sildenafil citrate (Viagra) is a potent inhibitor of the electrolytic enzyme type V phosphodiesterase (PDE5), in the corpus cavernosum and therefore increases the penile response to sexual stimulation...
- [Erectile dysfunction after radical prostatectomy : patient information, contact persons, postoperative proerectile therapy]S Kaufmann
Klinik für Urologie und Kinderurologie, Universitatsklinikum Schleswig Holstein, Campus Kiel, Campus Kiel, Arnold Heller Str 7, 24105, Kiel, Deutschland
Urologe A 49:525-9. 2010..the patients prior to the intervention about the risk of ED, which individuals the patients discuss this issue with, and whether the patients preoperatively consider use of a PDE5 inhibitor for proerectile therapy after the operation.
- Role of nitric oxide/cyclic GMP pathway in regulating spontaneous excitations in detrusor smooth muscle of the guinea-pig bladderYoshimasa Yanai
Department of Nephro urology, Nagoya City University Graduate School of Medical Sciences, Nagoya, Japan
Neurourol Urodyn 27:446-53. 2008..We have investigated the effects of NO donors and phosphodiesterase-5 (PDE5) inhibition on spontaneous excitations in DSM.
- Phosphodiesterase type 5 inhibitors in postprostatectomy erectile dysfunction: a critical analysis of the basic science rationale and clinical applicationKonstantinos Hatzimouratidis
2nd Department of Urology, Aristotle University, Thessaloniki, Greece
Eur Urol 55:334-47. 2009..Phosphodiesterase type 5 inhibitors (PDE5-Is) have recently been utilized not only as a treatment of ED in this population but also as a preventive strategy ..
- Phosphodiesterase inhibitors in the treatment of erectile dysfunction in spinal cord-injured menJ M Soler
Centre Bouffard Vercelli, Laboratoire d urodynamique et de sexologie, Cerbère, France
Spinal Cord 45:169-73. 2007..Open, before-after study...
- Effects of phosphodiesterase inhibitors on the inflammatory response of endothelial cells stimulated by myeloperoxidase-modified low-density lipoprotein or tumor necrosis factor alphaThierry Roumeguere
Laboratory of Experimental Medicine, Unit 222, CHU Charleroi, Free University of Brussels, Montigny le Tilleul, Belgium
Eur Urol 57:522-8. 2010Sildenafil, vardenafil, and tadalafil are phosphodiesterase type 5 inhibitors (PDE5-Is) usually used in the treatment of erectile dysfunction (ED)...
- Successful withdrawal of oral long-acting nitrates to facilitate phosphodiesterase type 5 inhibitor use in stable coronary disease patients with erectile dysfunctionGraham Jackson
Guy s and St Thomas Hospital Cardiothoracic Centre, London, United Kingdom
J Sex Med 2:513-6. 2005Vascular disease is the most common cause of male erectile dysfunction (ED). Phosphodiesterase type 5 (PDE5) inhibitors are effective in up to 80% of men but are contraindicated in the presence of oral nitrates, because of a potentially ..
- Time course of the interaction between tadalafil and nitratesRobert A Kloner
The Heart Institute, Good Samaritan Hospital, Cardiovascular Division, Keck School of Medicine, University of Southern California, Los Angeles, California 90017, USA
J Am Coll Cardiol 42:1855-60. 2003This study was designed to determine the time course of nitrate interaction with tadalafil, a phosphodiesterase 5 (PDE5) inhibitor with a half-life (t(1/2)) of 17.5 h.
- Phosphodiesterase 5 inhibitors in the treatment of premature ejaculationW F Wang
Department of Urology, Hainan Provincial People s Hospital, Haikou, Hainan Province, China
Int J Androl 29:503-09. 2006To date, there is no FDA-approved therapy for premature ejaculation (PE). Recently, phosphodiesterase 5 inhibitors (PDE5-Is) have been demonstrated to have encouraging results in the treatment of PE by a few studies...
- Molecular modeling studies of pyridopurinone derivatives--potential phosphodiesterase 5 inhibitorsP Srivani
Molecular Modeling Group, Organic Chemical Sciences, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India
J Mol Graph Model 26:378-90. 2007..QSAR) and docking studies were carried out on a series of pyridopurinones, to model their phosphodiesterase 5 (PDE5) inhibitory activities...
- Expression of the PDE5 enzyme on human retinal tissue: new aspects of PDE5 inhibitors ocular side effectsC Foresta
Department of Histology, Microbiology and Medical Biotechnologies, University of Padova, Padova, Italy
Eye (Lond) 22:144-9. 2008We tested the effect of two phosphodiesterase type-5 (PDE5) inhibitors, sildenafil and tadalafil, on ophthalmic artery (OA) blood flow velocity and investigated the presence of the PDE5 enzyme on human retinal tissue in comparison with ..
- Effects of phosphodiesterase-5 inhibitors on sperm parameters and fertilizing capacityF Dimitriadis
Department of Urology, Ioannina University School of Medicine, Ioannina 45110, Greece
Asian J Androl 10:115-33. 2008The aim of this review study is to elucidate the effects that phosphodiesterase 5 (PDE5) inhibitors exert on spermatozoa motility, capacitation process and on their ability to fertilize the oocyte...
- Effect of the phosphodiesterase 5 inhibitors sildenafil, tadalafil and vardenafil on rat anococcygeus muscle: functional and biochemical aspectsHaroldo A Toque
Department of Pharmacology, Faculty of Medical Sciences, UNICAMP, Campinas, Sao Paulo, Brazil
Clin Exp Pharmacol Physiol 36:358-66. 2009..The aim of the present study was to provide a functional and biochemical comparison of the three PDE5 inhibitors, namely sildenafil, tadalafil and vardenafil, in the rat anococcygeus muscle. 2...
- Chronic inhibition of phosphodiesterase 5 does not prevent pressure-overload-induced right-ventricular remodellingStefan Schafer
Cardiology Research, Bayer Schering Pharma, Aprather Weg 18, 42096 Wuppertal, Germany
Cardiovasc Res 82:30-9. 2009Inhibition of phosphodiesterase 5 (PDE5) decreases pulmonary pressure and improves symptoms in patients with pulmonary arterial hypertension...
- The ontogenetic expression pattern of type 5 phosphodiesterase correlates with androgen receptor expression in rat corpora cavernosaEleonora Carosa
Course of Endocrinology and Medical Sexology, Department of Experimental Medicine, University of L Aquila, L Aquila, Italy
J Sex Med 6:388-96. 2009..The mechanisms controlling erection in animals and in humans are mainly age-dependent. However, the ontogenesis of the biochemical machinery of erection is largely unknown...
- Microarray analysis of gene expression profile in the corpus cavernosum of hypercholesterolemic rats after chronic treatment with PDE5 inhibitorHan Gook Jung
Research Institutes of Dong A Pharmaceutical Company, 47 5 Sanggal, Kiheung, Youngin, Kyunggi 449 905, Republic of Korea
Life Sci 80:699-708. 2007..of hypercholesterolemia-related ED and to investigate the effects of Udenafil, a phosphodiesterase type 5 (PDE5) inhibitor, on gene expression, we performed microarray gene expression analysis via gene discovery methods using ..
- [3H]sildenafil binding to phosphodiesterase-5 is specific, kinetically heterogeneous, and stimulated by cGMPJackie D Corbin
Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, 702 Light Hall, Nashville, TN 37232 0615, USA
Mol Pharmacol 63:1364-72. 2003..acting as a nonhydrolyzable analog of cGMP and competing with this nucleotide for catalysis by phosphodiesterase-5 (PDE5), but the characteristics of direct binding of radiolabeled sildenafil to PDE5 have not been determined...
- cGMP catabolism by phosphodiesterase 5A regulates cardiac adrenergic stimulation by NOS3-dependent mechanismEiki Takimoto
Division of Cardiology, Department of Medicine, Johns Hopkins Medical Institutions, Baltimore, MD, USA
Circ Res 96:100-9. 2005..cGMP is also catabolically regulated by phosphodiesterase 5A (PDE5A)...
- Phosphodiesterase-5A dysregulation in penile erectile tissue is a mechanism of priapismHunter C Champion
Department of Cardiology, Johns Hopkins Hospital, 600 North Wolfe Street, Baltimore, MD 21287, USA
Proc Natl Acad Sci U S A 102:1661-6. 2005..We investigated the role of downstream guanylate cyclase and phosphodiesterase type 5 (PDE5A) expression and function in mediating these responses in eNOS-/- and nNOS-/-, eNOS-/- mice...
- The role of phosphodiesterase type 5 inhibitors in the management of premature ejaculation: a critical analysis of basic science and clinical dataJuza Chen
Department of Urology, Tel Aviv Sourasky Medical Center, Sackler Faculty of Medicine, Tel Aviv University, Tel Aviv, Israel
Eur Urol 52:1331-9. 2007To assess the usefulness of the phosphodiesterase type 5 inhibitors (PDE5-Is) in the treatment of premature ejaculation (PE) and to describe possible mechanisms to explain their effect.
- Critical amino acids in phosphodiesterase-5 catalytic site that provide for high-affinity interaction with cyclic guanosine monophosphate and inhibitorsRoya Zoraghi
Department of Molecular Physiology and Biophysics, 702 Light Hall, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 0615, USA
Biochemistry 46:13554-63. 2007The molecular bases for phosphodiesterase 5 (PDE5) catalytic-site affinity for cyclic guanosine monophosphate (cGMP) and potency of inhibitors are poorly understood...
- 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 stressI Russo
Diabetes Unit, Department of Clinical and Biological Sciences, University of Turin, San Luigi Gonzaga Hospital, 10043 Orbassano TO, Italy
Endocrinology 149:1480-9. 2008..and cGMP ability to induce, via PKG, vasodilator-stimulated phosphoprotein (VASP) phosphorylation at serine 239 and PDE5 activity; 3) protein expression of sGC, PKG, total VASP, and PDE5; 4) superoxide anion concentrations and ability ..
- Differential effects of the phosphodiesterase type 5 inhibitors sildenafil, vardenafil, and tadalafil in rat aortaCleber E Teixeira
Department of Physiology, Medical College of Georgia, Augusta, 30912 3000, USA
J Pharmacol Exp Ther 316:654-61. 2006Presumably, the vasorelaxant properties of phosphodiesterase type 5 (PDE5) inhibitors are similar in isolated blood vessels...
- In vitro effects of PDE5 inhibitors sildenafil, vardenafil and tadalafil on isolated human ureteral smooth muscle: a basic research approachChristian Gratzke
Department of Urology, Ludwig Maximilians University, University Hospital Grosshadern, Marchioninistr 15, 81377, Munich, Germany
Urol Res 35:49-54. 2007..The aim of the present study was to evaluate the functional effects of PDE5 inhibitors sildenafil (Sil), vardenafil (Var) and tadalafil (Tad), as well as nitric oxide (NO)-donating agent ..
- Pharmacological characterization of a novel phosphodiesterase type 5 (PDE5) inhibitor lodenafil carbonate on human and rabbit corpus cavernosumHaroldo A Toque
Department of Pharmacology, UNICAMP, Campinas, SP, 13081 970, Brazil
Eur J Pharmacol 591:189-95. 2008..Phosphodiesterase 5 (PDE5) inhibitors, such as sildenafil, prolong the NO effects by inhibiting cGMP breakdown...
- Synergy between natriuretic peptides and phosphodiesterase 5 inhibitors ameliorates pulmonary arterial hypertensionReshma S Baliga
Centre for Clinical Pharmacology, University College London, The Rayne Building, 5 University Street, London WC1E 5JJ, UK
Am J Respir Crit Care Med 178:861-9. 2008Phosphodiesterase 5 (PDE5) inhibitors (e.g., sildenafil) are selective pulmonary vasodilators in patients with pulmonary arterial hypertension...
- A placebo-controlled study of sildenafil effects on cognition in schizophreniaDonald C Goff
Department of Psychiatry, MGH Schizophrenia Program, Freedom Trail Clinic, Massachusetts General Hospital, Harvard Medical School, 25 Staniford St, 2nd Floor, Boston, MA, 02114, USA
Psychopharmacology (Berl) 202:411-7. 2009Phosphodiesterase 5 (PDE5) inhibitors increase cyclic guanosine monophosphate (cGMP) concentrations in the intracellular pathway activated by N-methyl-D-aspartic acid receptors which is believed to mediate long-term potentiation and ..
- The role of PDE5 inhibitors in heme oxygenase-cGMP relationship in rat cavernous tissuesM Talaat Abdel Aziz
Molecular Biology Unit, Medical Biochemistry Department, Faculty of Medicine, Cairo University, Cairo 11562, Egypt
J Sex Med 5:1636-45. 2008..Heme oxygenase (HO) enzyme catalyzes oxidative degradation of heme to biliverdin and carbon monoxide (CO). CO shares many properties with nitric oxide (NO) including the activation of soluble guanyl cyclase...
- Randomized phase II trial evaluation of erectile function after attempted unilateral cavernous nerve-sparing retropubic radical prostatectomy with versus without unilateral sural nerve grafting for clinically localized prostate cancerJohn W Davis
Department of Urology, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
Eur Urol 55:1135-43. 2009..Nonrandomized studies of unilateral nerve-sparing (UNS) radical prostatectomy (RP) have reported improved recovery of erectile function if the sacrificed cavernous nerve is reconstructed with a sural nerve graft (SNG)...
- Diabetes exacerbates the functional deficiency of NO/cGMP pathway associated with erectile dysfunction in human corpus cavernosum and penile arteriesJavier Angulo
Departamento de Investigacion, Hospital Ramon y Cajal, Madrid, Spain
J Sex Med 7:758-68. 2010Diabetic men with erectile dysfunction (ED) are less responsive to therapy with type 5 phosphodiesterase (PDE5) inhibitors...
- Allosteric-site and catalytic-site ligand effects on PDE5 functions are associated with distinct changes in physical form of the enzymeJackie D Corbin
Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 0615, United States
Cell Signal 21:1768-74. 2009Native phosphodiesterase-5 (PDE5) homodimer contains distinct non-catalytic cGMP allosteric sites and catalytic sites for cGMP hydrolysis. Purified recombinant PDE5 was activated by pre-incubation with cGMP...
- Does educational status affect a patient's behavior toward erectile dysfunction?Andrea Salonia
Department of Urology, University Vita Salute San Raffaele, Scientific Institute H San Raffaele, Milan, Italy
J Sex Med 5:1941-8. 2008..rarely as a potential factor affecting the behavior of patients with new onset erectile dysfunction (ED) toward seeking first medical help and subsequent compliance with prescribed phosphodiesterase type 5 inhibitor (PDE5) therapy.
- Co-possession of phosphodiesterase type-5 inhibitors (PDE5-I) with nitratesLi Ling Chang
IMS Health, Inc, Plymouth Meeting, PA 19422, USA
Curr Med Res Opin 26:1451-9. 2010Estimate the proportion of phosphodiesterase type-5 inhibitor (PDE5-I) patients who co-possess nitrates and compare the proportion of tadalafil patients dispensed nitrates to a matched control group...
- Vardenafil can improve continence recovery after bilateral nerve sparing prostatectomy: results of a randomized, double blind, placebo-controlled pilot studyMauro Gacci
Department of Urology, University of Florence, Careggi Hospital, Florence, Italy
J Sex Med 7:234-43. 2010Phosphodiesterase type 5 inhibitors (PDE5-I) have acquired an established role in the treatment of post-prostatectomy erectile dysfunction (ED)...
- The role of PDE5-inhibitors in cardiopulmonary disorders: from basic evidence to clinical developmentMarco Guazzi
Department of Medicine, Surgery and Dentistry, University of Milan, San Paolo Hospital, Milan, Italy
Curr Med Chem 14:2181-91. 2007..g., cGMP and cAMP. PDE isoenzyme 5 (PDE5) is specifically involved in cGMP inactivation in the smooth muscle cell...
- Phosphodiesterase type 5 inhibition coupled to strong reinforcement results in two periods of transient retention loss in the young chickT M Edwards
School of Psychology, Psychiatry and Psychological Medicine, Monash University, Wellington Rd, Clayton, Victoria 3800, Australia
Behav Brain Res 183:231-5. 2007Previous behavioural studies which have administered phosphodiesterase type-5 (PDE5) inhibitors have consistently demonstrated improved retention...
- Increased cardiac myocyte PDE5 levels in human and murine pressure overload hypertrophy contribute to adverse LV remodelingSara Vandenwijngaert
Department of Cardiovascular Sciences, KU Leuven, Leuven, Belgium
PLoS ONE 8:e58841. 2013..We examined expression of phosphodiesterase 5 (PDE5), an enzyme that hydrolyzes cGMP, in human and mouse hearts subjected to sustained left ventricular (LV) pressure ..
- Effect of nitric oxide on the cyclic guanosine monophosphate (cGMP) pathway during meiosis resumption in bovine oocytesKátia R Lancellotti Schwarz
Departamento de Medicina Veterinaria, Faculdade de Zootecnia e Engenharia de Alimentos, Universidade de Sao Paulo, Pirassununga SP, Brazil
Theriogenology 81:556-64. 2014..Also, to our knowledge this is the first report to detect PKG1, PKG2, phosphodiesterase-5A, ADCY3, ADCY6, and ADCY9 transcripts in bovine oocytes. ..
- Pomegranate juice causes a partial improvement through lowering oxidative stress for erectile dysfunction in streptozotocin-diabetic ratE Onal
Departments of Pharmacology and Biochemistry, Faculty of Pharmacy, Ankara University, Ankara, Turkey
Int J Impot Res 28:234-240. 2016..Our results highlight the success of antioxidant mechanism of PJ in ED with diabetes and open the way for future understanding in alternative treatment combinations with PDE5 inhibitors.
- Novel alternative splice variants of cGMP-binding cGMP-specific phosphodiesteraseJ Kotera
Discovery Research Laboratory, Tanabe Seiyaku Co Ltd, 2 50, Kawagishi 2 chome, Toda, Saitama, 335 8505, Japan
J Biol Chem 273:26982-90. 1998..Thus, two types of alternative splice variants of canine cGB-PDE have been identified and shown to have similar biological properties in vitro...
- [The endocrine basis of sexual dysfunction in the elderly]W Krause
Arbeitskreis Andrologie der Deutschen Dermatologen AAD, Abteilung Andrologie, Dermatologische Klinik, Klinikum der Philipps Universität, Marburg
Urologe A 39:411-3. 2000..In an animal experiment, the intracavernous pressure, the density of alpha-receptors, and the PDE5 activity depended on normal testosterone levels...
- Physiological significance of nitrergic transmission in human penile erectionP G Adaikan
Department of Obstetrics and Gynaecology, National University Hospital, National University of Singapore, Lower Kent Ridge Road, Singapore 119 074
Asian J Androl 2:51-6. 2000..This causes relaxation of CC muscle. Phosphodiesterase type 5 (PDE5) is responsible for the degradation of cGMP and regulation of CC muscle tone...
- Characterization of human, dog and rabbit corpus cavernosum type 5 phosphodiesterasesP Wang
Schering Plough Research Institute, Kenilworth, NJ 07033, USA
Life Sci 68:1977-87. 2001Human, dog and rabbit corpus cavernosum type 5 phosphodiesterases (PDE5) were isolated and their characteristics were compared. The three enzymes showed Km values of 0.8, 2.1 and 2.3 uM, respectively...
- Absence of clinically important HERG channel blockade by three compounds that inhibit phosphodiesterase 5--sildenafil, tadalafil, and vardenafilR Dustan Sarazan
Lilly Research Laboratories, Eli Lilly and Company, 2001 W Main St, Greenfield, Indianapolis, IN 46140, USA
Eur J Pharmacol 502:163-7. 2004Compounds that inhibit phosphodiesterase 5 (PDE5) have been developed for the treatment of erectile dysfunction...
- The effect of PDE5 inhibition on the erectile function in streptozotocin-induced diabetic ratsG J Ahn
Department of Efficacy and Toxicology, Preclinical Division, Research Laboratories, Dong A Pharmaceutical Company Ltd, Kyunggi, Republic of Korea
Int J Impot Res 17:134-41. 2005..87+/-2272 in diabetic group). These results suggest that subchronic treatment of DA-8159 can prevent the development of erectile dysfunction (ED), and provides a rationale for the use of DA-8159 as treatment of diabetic ED...
- Phosphodiesterase 5 enzyme and its inhibitors: update on pharmacological and therapeutical aspectsS K Kulkarni
Pharmacology Division, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India
Methods Find Exp Clin Pharmacol 26:789-99. 2004..Phosphodiesterase type 5 (PDE5) is one of the members of the superfamily that specifically cleaves cyclic guanosine monophosphate (cGMP), a key ..
- Clinical monograph for drug formulary review: erectile dysfunction agentsHelen Eloise Campbell
WellPoint Pharmacy Management, PO Box 9, Cherry Valley, NY, 13320, USA
J Manag Care Pharm 11:151-71. 2005..in recent years, most notably the introduction of sildenafil, the first oral selective phosphodiesterase type 5 (PDE5) inhibitor, in 1998...
- In vitro inhibition of human cGMP-specific phosphodiesterase-5 by polyphenols from red grapesMario dell'Agli
Department of Pharmacological Sciences, Faculty of Pharmacy, University of Milan, Via Balzaretti 9, 20133 Milan, Italy
J Agric Food Chem 53:1960-5. 2005..wine-derived phenolic compounds was associated with the inhibition of phosphodiesterases (PDEs) and, in particular, PDE5. For this purpose, human recombinant PDE5A1 isoform was prepared by expression of the full-length cDNA of PDE5A1 ..
- Effects of combined treatment with sildenafil and itraconazole on the cardiovascular system in telemetered conscious dogsEun Joo Kim
Department of Pharmacology and National Research Laboratory, Korea Institute of Toxicology, Korea Research Institute of Chemical Technology, Yuseong, Daejeon, Korea
Drug Chem Toxicol 28:177-86. 2005Sildenafil, a potent PDE5 inhibitor, is widely prescribed as a treatment of erectile dysfunction. Itraconazole is an inhibitor of CYP3A4, a metabolic enzyme of sildenafil...
- Life after PDE4: overcoming adverse events with dual-specificity phosphodiesterase inhibitorsMark A Giembycz
Department of Pharmacology and Therapeutics, Institute of Infection, Immunity and Inflammation, University of Calgary, 3330 Hospital Drive NW, Calgary, Alberta, Canada, T2N 4N1
Curr Opin Pharmacol 5:238-44. 2005..The development of dual-specificity compounds that inhibit PDE4 and PDE1, PDE3, PDE5 or PDE7 could be beneficial for the treatment of chronic inflammatory lung diseases and are currently being ..
- [Cost of fertility and erectile dysfunction therapy: who has to pay what in the GVK?]I Schroeder-Printzen
Universitätsklinikum Giessen und Marburg, Giessen
Urologe A 44:1179-82. 2005..Before 2004 medical therapy of erectile dysfunction (autoinjection therapy, PDE5 inhibitors) was included in the coverage of the general health insurance; however, it is now excluded by law...
- Long-term treatment of erectile dysfunction with a phosphodiesterase-5 inhibitor and dose optimization based on nocturnal penile tumescenceMichael J Mathers
Urological Ambulatory Remscheid, Remscheid, Germany
BJU Int 101:1129-34. 2008To test the hypothesis that a variable dosage of the oral phosphodiesterase type 5 (PDE5) inhibitor sildenafil (25, 50, 100 mg) or vardenafil (5, 10, 25 mg) determined according to results obtained from nocturnal penile tumescence and ..
- Effect of nightly versus on-demand vardenafil on recovery of erectile function in men following bilateral nerve-sparing radical prostatectomyFrancesco Montorsi
Division of Urology, Universita Vita Salute San Raffaele, Via Olgettina 60, Milan, Italy
Eur Urol 54:924-31. 2008..data have been available from large, well-designed trials comparing on demand and nightly dosing of phosphodiesterase type 5 (PDE5) inhibitors on recovery of erectile function in postprostatectomy patients with erectile dysfunction (ED).
- Aspects of sexual satisfaction in men with erectile dysfunction: a factor analytic and logistic regression approachAxel Fugl-Meyer
University of Uppsala Neuroscience, Rehabilitation Medicine, Upssala, Sweden
J Sex Med 6:232-42. 2009..Index of Erectile Function (IIEF), Sexual Encounter Profile (SEP), and Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) assess efficacy of phosphodiesterase type 5 (PDE5) inhibitor treatment of erectile dysfunction (ED).
- Combined use of PDE5 inhibitors and nitrates in the treatment of pulmonary arterial hypertension in patients with heart failureJosef Stehlik
Cardiology Section, VA Salt Lake City Health Care System, Salt Lake City, UT 84148, USA
J Card Fail 15:31-4. 2009Phosphodiesterase-5 (PDE5) inhibitors, which induce relaxation of smooth muscle with some selectivity for the pulmonary vasculature, are used in the treatment of pulmonary hypertension...
- Lack of direct androgen regulation of PDE5 expressionRong Yang
Knuppe Molecular Urology Laboratory, Department of Urology, School of Medicine, University of California, 533 Parnassus Ave, Box 0738, San Francisco, CA 94143 0738, USA
Biochem Biophys Res Commun 380:758-62. 2009..Prostate specific antigen (PSA) promoter activity was upregulated while PDE5A promoter activity remained unchanged in DHT-treated CSMC...
- Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring systemRobert O Hughes
Pfizer Global Research and Development, Chesterfield Parkway West, St Louis, MO 63017, USA
Bioorg Med Chem Lett 19:4092-6. 2009Efforts to improve the potency and physical properties of the aminopyridiopyrazinone class of PDE5 inhibitors through modification of the core ring system are described...
- Phosphodiesterase 5 inhibition improves synaptic function, memory, and amyloid-beta load in an Alzheimer's disease mouse modelDaniela Puzzo
Department of Pathology and Cell Biology and Taub Institute for Research on Alzheimer s Disease and the Aging Brain, Columbia University Medical Center, New York, New York 10032, USA
J Neurosci 29:8075-86. 2009..Here, we report that the phosphodiesterase 5 inhibitor (PDE5) sildenafil (Viagra), a molecule that enhances phosphorylation of CREB, a molecule involved in memory, through ..
- Acute hemodynamic effects of intravenous sildenafil citrate in congestive heart failure: comparison of phosphodiesterase type-3 and -5 inhibitionPhil Botha
Department of Cardiopulmonary Transplantation, Freeman Hospital, Newcastle upon Tyne, United Kingdom
J Heart Lung Transplant 28:676-82. 2009..The phosphodiesterase 3 (PDE3) and PDE5 inhibitors both increase levels of cyclic nucleotides in the vascular smooth muscle, causing vasodilatation...
- [Vardenafil for refractory erectile dysfunction: the latest advances]Hao Yang Wang
Department of Reproduction and Genetics, PLA Research Institute of Clinical Laboratory Medicine, Nanjing General Hospital of Nanjing Military Region, Nanjing, Jiangsu 210002, China
Zhonghua Nan Ke Xue 15:1035-8. 2009In recent years, more and more attention has been drawn to the role of phosphodiesterase 5 (PDE5) in penile erection...
- Phosphodiesterase-5 gene (PDE5A) polymorphisms are associated with progression of childhood IgA nephropathyWon Ho Hahn
Department of Pediatrics, East West Kidney Diseases Research Institute, School of Medicine, Kyung Hee University, Hoegi dong 1, Dongdaemun Gu, Seoul 130 702, Korea
Pediatr Nephrol 25:1663-71. 2010..The present study was conducted to investigate the association among 16 single nucleotide polymorphisms (SNPs) of PDE5A and childhood IgAN...
- [Treatment of pulmonary arterial hypertension]Xavier Jais
Universite Paris Sud XI, Orsay, France
Presse Med 39:1S22-32. 2010..with epoprostenol and either an endothelin-receptor antagonist (ERA) or a phosphodiesterase type 5 inhibitor (PDE5 I), or both should also be discussed...
- Avanafil, a new rapid-onset phosphodiesterase 5 inhibitor for the treatment of erectile dysfunctionMa Limin
Tulane University, Health Sciences Center, Department of Urology, 1430 Tulane Avenue, SL 42, New Orleans, LA 70112, USA
Expert Opin Investig Drugs 19:1427-37. 2010..Phosphodiesterase type 5 (PDE5) inhibitors (sildenafil, tadalafil and vardenafil) are currently the first-line treatment option presented to ..
- Vardenafil decreases bladder afferent nerve activity in unanesthetized, decerebrate, spinal cord-injured ratsDelphine Behr-Roussel
Pelvipharm, Orsay, France
Eur Urol 59:272-9. 2011Phosphodiesterase type 5 inhibitors (PDE5-Is) improve storage symptoms in benign prostatic hyperplasia patients, despite a lack of effect on peak urinary flow rate...
- GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterizationCathy J Tralau-Stewart
Drug Discovery Institute, Faculty of Medicine, Imperial College London, London, United Kingdom
J Pharmacol Exp Ther 337:145-54. 2011..GSK256066 was highly selective for PDE4 (>380,000-fold versus PDE1, PDE2, PDE3, PDE5, and PDE6 and >2500-fold against PDE7), inhibited PDE4 isoforms A-D with equal affinity, and had a substantial ..
- [Phosphodiesterase regulation of cardiovascular functions]La Li
Department of Physiology and Pathophysiology, Peking University Health Science Center, Beijing 100191, China
Sheng Li Ke Xue Jin Zhan 41:100-6. 2010..The functions of blood vessels are regulated by the reactivity and phenotypes of vascular smooth muscle. PDE5 inhibitors, by enhancing the vasodilator effect of cGMP, have been successfully applied to the treatment of ..
- Treatment of erectile dysfunction and lower urinary tract symptoms by phosphodiesterase inhibitorsStefan Uckert
Division of Surgery, Department of Urology and Urological Oncology, Hannover Medical School, 30625 Hannover, Germany
Handb Exp Pharmacol . 2011..symptoms of lower urinary tract dysfunction is now widely accepted following the successes of phosphodiesterase 5 (PDE5) inhibitor treatment of erectile dysfunction, the treatment of urological diseases has focused on orally available ..
- Non-invasive management of primary phosphodiesterase type 5 inhibitor failure in patients with erectile dysfunctionGregory Lowe
Department of Urology, Ohio State University Medical Center, Columbus, OH, USA
Ther Adv Urol 1:235-42. 2009Phosphodiesterase type 5 inhibitors (PDE5-i) have become first line therapy for the treatment of erectile dysfunction. Most initial prescriptions for PDE5-i are by primary care practitioners...
- [Effects and mechanisms of phosphodiesterase type 5 inhibitors on rats with overactive bladder]Hong de Chen
Department of Urology, Wenzhou Medical College, Wenzhou, China
Zhonghua Yi Xue Za Zhi 91:2001-5. 2011To investigate the effects and the possible mechanistic pathway of phosphodiesterase type 5 (PDE5) inhibitors on rats with overactive bladder.
- Recurrent uveitis due to sildenafil usage in a patient with Behçet's diseaseMetin Isik
Department of Internal Medicine, Hacettepe University Hospital, Sihhiye, Ankara, Turkey
Rheumatol Int 33:803. 2013..Sildenafil (Viagra(R)) and the other phosphodiesterase type 5 (PDE5) inhibitors are the first-line options for the treatment of erectile dysfunction, but transient visual symptoms and ..
- Does current scientific and clinical evidence support the use of phosphodiesterase type 5 inhibitors for the treatment of premature ejaculation? a systematic review and meta-analysisAnastasios D Asimakopoulos
UOC of Urology, Department of Surgery, University of Tor Vergata, Policlinico Casilino, Rome, Italy
J Sex Med 9:2404-16. 2012..Premature ejaculation (PE) is a highly prevalent and complex syndrome that remains poorly defined and inadequately characterized. Pharmacotherapy represents the current basis of lifelong PE treatment...
- cGMP-Prkg1 signaling and Pde5 inhibition shelter cochlear hair cells and hearing functionMirko Jaumann
University of Tubingen, Department of Otolaryngology, Tübingen Hearing Research Centre, Molecular Physiology of Hearing, Tubingen, Germany
Nat Med 18:252-9. 2012..mice, and its expression partly overlapped with the expression profile of cGMP-hydrolyzing phosphodiesterase 5 (Pde5)...
- Ca2+ -activated K+ channel (KCa) stimulation improves relaxant capacity of PDE5 inhibitors in human penile arteries and recovers the reduced efficacy of PDE5 inhibition in diabetic erectile dysfunctionR Gonzalez-Corrochano
Servicio de Histología Investigación, Instituto Ramón y Cajal de Investigación Sanitaria, Hospital Universitario Ramon y Cajal, Madrid, Spain
Br J Pharmacol 169:449-61. 2013..calcium-activated potassium channels (KCa ) activation on cGMP-mediated relaxation in human penile tissues from non-diabetic and diabetic patients, and on the effects of PDE5 inhibitors on erectile responses in control and diabetic rats.
- Selective inhibition of phosphodiesterase 5 enhances glutamatergic synaptic plasticity and memory in miceSubramaniam Uthayathas
Department of Pharmacal Sciences, Harrison School of Pharmacy, Auburn University, Auburn, Alabama Department of Pharmacology, Howard University College of Medicine, Washington, DC
Synapse 67:741-7. 2013Phosphodiesterases (PDEs) belong to a family of proteins that control metabolism of cyclic nucleotides. Targeting PDE5, for enhancing cellular function, is one of the therapeutic strategies for male erectile dysfunction...
- The molecular basis for the selectivity of tadalafil toward phosphodiesterase 5 and 6: a modeling studyYi You Huang
School of Pharmaceutical Sciences, Sun Yat Sen University, Guangzhou 510006, China
J Chem Inf Model 53:3044-53. 2013Great attention has been paid to the clinical significance of phosphodiesterase 5 (PDE5) inhibitors, such as sildenafil, tadalafil, and vardenafil widely used for erectile dysfunction...
- In-vitro effects of PDE5 inhibitor and statin treatment on the contractile responses of experimental MetS rabbit's cavernous smooth muscleYasin Erden
Cumhuriyet University School of Medicine Department of Urology
Arch Ital Urol Androl 86:33-8. 2014....
- Regulation of OSU-03012 toxicity by ER stress proteins and ER stress-inducing drugsLaurence Booth
Department of Biochemistry and Molecular Biology, Virginia Commonwealth University, Richmond, Virginia
Mol Cancer Ther 13:2384-98. 2014..examined the toxic interaction between the non-coxib celecoxib derivative OSU-03012 and phosphodiesterase 5 (PDE5) inhibitors, and also determined the roles of endoplasmic reticulum stress response regulators in cell survival...
- Somatic amplifications and deletions in genome of papillary thyroid carcinomasNadia Passon
Azienda Ospedaliero Universitaria S Maria della Misericordia, Udine, Italy
Endocrine 50:453-64. 2015..Most frequent amplifications were detected at regions 2q35, 4q26, and 4q34.1, containing FN1, PDE5A, and GALNTL6 genes, respectively. Most frequent deletions occurred at regions 6q25...
- Reduced vascular responses to soluble guanylyl cyclase but increased sensitivity to sildenafil in female rats with type 2 diabetesStyliani Goulopoulou
Department of Physiology, Georgia Regents University, Augusta, Georgia
Am J Physiol Heart Circ Physiol 309:H297-304. 2015..82 ± 0.07 vs. 10.27 ± 0.08, P < 0.05) and increased sensitivity to sildenafil [phosphodiesterase 5 (PDE5) inhibitor; pEC50: 7.89 ± 0.14 vs. 8.25 ± 0.13, P < 0.05]...
- Novel Therapeutic Strategies for Reducing Right Heart Failure Associated Mortality in Fibrotic Lung DiseasesAyodeji Adegunsoye
Section of Pulmonary and Critical Care Medicine, Department of Medicine, University of Chicago, Chicago, IL 60637, USA
Biomed Res Int 2015:929170. 2015..calcium channel blockers, endothelin (ET-1) receptor antagonists, prostacyclin analogs, phosphodiesterase type 5 (PDE5) inhibitors, and rho-kinase (ROCK) inhibitors...
- cGMP Phosphodiesterase Inhibitors in a Mouse Model of Duchenne Muscular DystrophySTANLEY FROEHNER; Fiscal Year: 2009..PDE inhibitors, particularly those targeted at PDE5, reduce cardiac hypertrophy and fibrosis in a pressure induced mouse model...
- DAVID ALAN KASS; Fiscal Year: 2016..This has led to two major NIH- sponsored multicenter trials of PDE5 inhibitors in heart failure with either reduced or preserved ejection fraction...
- Rick H Cote; Fiscal Year: 2016..Furthermore, the increasing therapeutic reliance on PDE5 inhibitors (e.g...
- Structure and Regulation of the GPCR-G Protein Interactions in the Visual SystemARNOLD EINO RUOHO; Fiscal Year: 2011..spectrometry analysis;(c) The NMR solution structure of the full-length PDEg complexed with the catalytic core of a PDE5/6 chimera will be determined using 2H/13C/15N labeled proteins...
- A Novel HTS Cell-Based Assay For Cyclic GMPGary Piazza; Fiscal Year: 2007..protein composed of cyan- and yellow fluorescent proteins (CFP/YFP) fused with the cGMP binding domain of PDE2 or PDE5. Fluorescence resonance energy transfer (FRET) results from a conformational change of the protein upon cGMP ..
- NITRIC OXIDE AND IN VIVO BRAIN ARTERIOLAR RELAXATIONDale Pelligrino; Fiscal Year: 2004..3 principal PDEs found in cerebral VSM-the cAMP-"preferring" PDE3, the cAMP-specific PDE4, and the cGMP-specific PDE5. Primary increases in endogenous cAMP and cGMP production will be elicited by the adenylyl and guanylyl cyclase ..
- REGULATION OF PDE 5 IN HUMAN PENILE SMOOTH MUSCLE CELLSNoel Kim; Fiscal Year: 2001..function in men with impotence, resulting from a broad range of etiologies, emphasizes the crucial aspect which PDE5 plays in regulating penile smooth muscle tone...
- Peptide Therapy for Pulmonary Arterial HypertensionJawaharlal M Patel; Fiscal Year: 2013..Alternatively, pulmonary vascular cGMP levels can also be elevated via inhibition of phosphodiesterase type 5 (PDE5) to achieve a similar response...
- Planning a Multicenter Trial of PDE5A Inhibition for Duchenne Muscular DystrophyRonald G Victor; Fiscal Year: 2012..Indeed, phosphodiesterase (PDE5A) inhibitors, which prolong the half-life of cGMP-the downstream target of NO in vascular smooth muscle-rapidly ..
- Nancy J Brown; Fiscal Year: 2014..In contrast, three-week treatment with the phosphodiesterase 5 (PDE5) inhibitor tadalafil improves beta cell function in subjects with the metabolic syndrome without altering ..
- PITCH HF (CCC) Lead ApplicationMarc J Semigran; Fiscal Year: 2013..will be the first trial to assess the effect of a selective pulmonary vasodilator, the type 5 phosphodiesterase (PDE5) inhibitor tadalafil, on long-term clinical outcomes in heart failure (HF) patients with left ventricular (LV) ..
- Preeclampsia, IUGR and Hypertension: Targets for TreatmentJoey P Granger; Fiscal Year: 2013..Based on our exciting preliminary data, we propose to test the central hypothesis that PDE5 inhibitors attenuate the blood pressure and renal responses to placental ischemia in pregnant rats by inhibition of ..
- Kathryn N Farrow; Fiscal Year: 2016..dysregulation in the pulmonary vasculature are soluble guanylate cyclase (sGC) and phosphodiesterase 5 (PDE5)...
- Regulation and function of cGMP dependent protein kinase in cardiac hypertrophyEiki Takimoto; Fiscal Year: 2013..We recently found that blocking cGMP degradation with phospho- diesterase5A (PDE5A) inhibitor have potent anti-hypertrophic and anti-remodeling effects...
- PITCH HF (DCC)Flora Sandra Siami; Fiscal Year: 2013..will be the first trial to assess the effect of a selective pulmonary vasodilator, the type 5 phosphodiesterase (PDE5) inhibitor tadalafil, on long-term clinical outcomes in heart failure (HF) patients with left ventricular (LV) ..
- PDE5A Inhibition Stimulates Stem Cell Survival &DifferentiationMuhammad Ashraf; Fiscal Year: 2013..To address this, we propose the following four hypotheses. Hypothesis 1: Suppression of PDE5A using a long acting inhibitor, Tadalafil, will promote MSCs survival, engraftment and angiomyogenic ..
- Nitric Oxide/cGMP Modulation of Corporal Fibrosis Caused by NeuropraxiaMONICA GABRIELA FERRINI; Fiscal Year: 2012..induced by BCNR/BCNC can be prevented pharmacologically by the continuous and long-term administration of either PDE5 inhibitors, which increases intracorporeal NO and cGMP...
- Regulation, interaction, and inhibitor discovery of phosphodiesterasesHengming Ke; Fiscal Year: 2013..Selective inhibitors of PDEs have been studied as therapeutic agents for various human diseases. An example is PDE5-selective inhibitor sildenafil (Viagra) that is a drug for treatment of erectile dysfunction and pulmonary ..
- CELLULAR BIOLOGY OF RENAL FUNCTION AND DISEASEDennis Brown; Fiscal Year: 2012..A novel role for AQP2 in regulating actin polymerization via interaction with RhoGAPS will be explored. Use of PDE5 inhibitors and statins to achieve VP-independent urine concentration will be tested as a potential strategy for ..
- Mark T Nelson; Fiscal Year: 2016..corpus tissue will be addressed in Aim 2, which will also consider the role of the cGMP-specific phosphodiesterase, PDE5, and Ca2+-sensitive chloride currents (ClCa) as potential contributors to tissue-specific differences in NO ..
- Novel Peptide for Dynamic Regulation of Lung Endothelium NOS/cGMP FunctionsJawaharlal M Patel; Fiscal Year: 2011..Alternatively, pulmonary vascular cGMP levels can also be elevated via inhibition of phosphodiesterase type 5 (PDE5) to achieve a similar response...
- Role of calcium sensitization in diabetes-induced erectile dysfunctionMICHAEL EDWARD DISANTO; Fiscal Year: 2010..Although efficacious orally active PDE5 inhibitors have been developed to treat ED, a large percentage of diabetic men (with estimates as high as 50%) ..
- PDE5i with Tadalafil Changes the Extent of Renal Damage (PITCH_ER)Ravi Thadhani; Fiscal Year: 2013..study provides an efficient, economical, and well-powered approach to identify potential renoprotective effects of PDE5 inhibition...
- Gary A Piazza; Fiscal Year: 2016..NSAIDs such as sulindac sulfide (SS) are closely associated with inhibition of the cGMP-specific phosphodiesterase, PDE5. SS can selectively inhibit PDE5 to increase intracellular cGMP levels and activate protein kinase G to ..
- S MURTHY KARNAM; Fiscal Year: 2016..are regulated via feedback phosphorylation of cyclases (AC V/VI and sGC) and phosphodiesterases (PDE3A, PDE4D5, and PDE5) by PKA and PKG...
- Dennis Brown; Fiscal Year: 2016..Aim 2 will first expand our promising work on phosphodiesterase (PDE5) inhibitors, calcitonin and statins, which promote AQP2 membrane accumulation and increase urine concentration...
- MicroRNA, sulindac, and breast cancer chemopreventionYaguang Xi; Fiscal Year: 2013..MiR-200b can reduce the expression of the cGMP-specific phosphodiesterase PDE5, which has been previously reported to be overexpressed in tumor cells and closely associated with the apoptosis-..
- Lei Wang; Fiscal Year: 2015..The phosphodiesterase-5 (PDE5) enzyme is highly specific for hydrolysis of cGMP...
- The role of myeloid suppressor cells in tumor-specific toleranceIvan M Borrello; Fiscal Year: 2011..We will also examine the role of PDE5 inhibitors such as sildenafil in abrogating MSC function and test various therapeutic conditions in an effort to ..
- BRIAN RICHARD LINDMAN; Fiscal Year: 2015..Emerging preclinical and clinical data suggest that phosphodiesterase type 5 (PDE5) inhibition may help in this regard...
- Novel PDE5 inhibitors as a therapeutic tool against Alzheimer's DiseaseOttavio Arancio; Fiscal Year: 2013..Most importantly, sildenafil, an inhibitor of the cGMP-degrading enzyme phosphodiesterase V (PDE5), one of the components of the pathway, ameliorates synaptic and memory abnormalities in an amyloid-depositing ..
- Epsilon-sarcoglycan in LGMD Type 2DKevin Campbell; Fiscal Year: 2009..Significantly, we found that pharmacological treatment with PDE5A inhibitors relieves this form of fatigue by enhancing the nitric oxide signaling from active muscle...
- Basic Investigations in Brain RemodelingZheng Gang Zhang; Fiscal Year: 2011Treatment of stroke with a selective inhibitor of phosphodiesterase type 5 (PDE5), e.g...
- Sonic hedgehog, a regulator of CN injury induced apoptosisCAROL ANN PODLASEK; Fiscal Year: 2012..30-87% of prostate cancer patients treated by prostatectomy experience ED and PDE5 inhibitors are ineffective in 29-86% of prostatectomy patients who experience ED, depending on their nerve injury ..
- BASIS FOR RENAL RESISTANCE TO ATRIAL NATRIURETIC PEPTIDEMichael Humphreys; Fiscal Year: 2004..We shall determine the role of heightened PDE5 activity in the renal resistance to ANP observed in rats with experimental nephrosis or liver cirrhosis by (1) ..
- ERECTILE DYSFUNCTION AND NITRIC OXIDE SYNTHASE IN AGINGNestor Gonzalez Cadavid; Fiscal Year: 2006..Failure to respond to PDE5 inhibitors may be related to these factors. The overall ...
- PDE5 Inhibition Modulates Right Ventricular FailureAnna Hemnes; Fiscal Year: 2006..guanylyl cyclase in response to stimulation by nitric oxide, and is cleared by phosphodiesterases, including PDE5A. Expression of PDE5A has been found in cardiomyocytes...
- Molecular Mechanisms of PDE5 RegulationJackie Corbin; Fiscal Year: 2005..The subject of this application is the cGMP-binding cGMP-specific PDE (PDE5), which is specific for cGMP over cAMP at its allosteric cGMP-binding sites and at its catalytic site...
- Molecular Control of cGMP Signaling by PKGs and PDEsJackie Corbin; Fiscal Year: 2007..cGMP effects are cGMP-dependent protein kinase (PKG), cGMP-gated ion channel proteins, cGMP-binding PDEs (PDE2, PDE5, PDE6, PDE 10, PDE11), and cAMP-dependent protein kinase (PKA) by cross-activation...
- COLLABORATIVE R01-CARDIAC GRAFTS-FUNCTIONAL ANALYSESRobert Kloner; Fiscal Year: 2003....
- Biologic Ventricular Assist DeviceRobert Kloner; Fiscal Year: 2004..Identification and characterization of transplants will be carried out with PCR analysis of the Y chromosome (male cells into female host), detailed histologic analysis and immunostaining for muscle cell markers. ..
- Mesenchymal Stem Cells for Myocardial InfarctionRobert Kloner; Fiscal Year: 2006..abstract_text> ..
- Tadalafil Induced Modulation of Immune Response in HNSCCJoseph A Califano; Fiscal Year: 2010..anergy in both CD4+ and CD8+ T-cells in HNSCC, and that functional elimination of MDSCs via phosphodiesterase 5 (PDE5) inhibitors can restore T cell function in lymphocytes from HNSCC patients...
- NITRIC OXIDE REGULATORY SYSTEM IN THE PENISArthur Burnett; Fiscal Year: 2002....
- 2008 AUA/SBUR Summer Research ConferenceArthur Burnett; Fiscal Year: 2008..unreadable] [unreadable] [unreadable]..
- Role of Stretch to Endothelial Pulse-Perfusion ResponseDavid Kass; Fiscal Year: 2005..abstract_text> ..
- Cardiovascular Stiffening in Aged Patients with CHFDavid Kass; Fiscal Year: 2005..This could lead to new therapeutic approaches to this difficult clinical problem that affects a growing aged patient population. ..
- EXCITATORY AMINO ACIDS IN GLAUCOMAAlan Laties; Fiscal Year: 2004..These experiments will help test the central hypothesis--for if one can block the effects of IOP elevation with glutamate antagonists, then elevated 10P may toxic glutamate levels ganglion cell loss. ..
- Poly(ADP-ribose)Polymerase & Doxorubicin CardiotoxicityJon Mabley; Fiscal Year: 2002..PROPOSED COMMERCIAL APPLICATIONS: The annual anticipated revenues for an effective therapeutic to prevent anti-cancer-drug induced cardiodepression is over $100 million in the US alone. ..
- Lower urinary tract dysfunction in Parkinson's diseaseNaoki Yoshimura; Fiscal Year: 2003..This is a high priority in the urologic care of patients with Parkinson's disease. ..
- SIGNALING MECHANISMS IN PHARMACOLOGICAL PRECONDITIONINGRAKESH KUKREJA; Fiscal Year: 2004..These studies will help us learn a great deal on the endogenous mechanisms of delayed preconditioning and assist us in developing innovative techniques leading to one of the most effective means of salvaging ischemic myocardium. ..
- Bladder Pain Gene Therapy with Pro-opiomelanocortin cDNANaoki Yoshimura; Fiscal Year: 2004..This research project is important to provide a solid basis for potential future clinical application. ..
- Myicardial injury: role of poly (ADP-ribose) synthetaseCsaba Szabo; Fiscal Year: 2005..Further, based on exciting preliminary data, the final, fifth aim is focusing in establishing the role of PARS in myocardial preconditioning. ..
- Afferent modulation in bladde dysfunctionNaoki Yoshimura; Fiscal Year: 2007..abstract not provided ..
- Study of Intrinsic Bladder Activity by Optical ImagingAnthony Kanai; Fiscal Year: 2007..To study the neural-chemical control of spontaneous detrusor activity; and III.) To determine the origin of detrusor overactivity in partially obstructed bladders. ..
- INFLAMMATION & CORTICOSTEROID RESPONSES IN SEVERE ASTHMAKIAN CHUNG; Fiscal Year: 2005..The molecular mechanisms underlying loss of CR will be examined. These studies should lead to more effective therapies for chronic severe asthma. ..
- Molecular Anatomy of Mitochondria in HNSCJoseph Califano; Fiscal Year: 2006..Ultimately, identified mitochondrial alterations will be used as markers for molecular detection approaches using a novel, fluorescence based gap ligase chain reaction assay. [unreadable] [unreadable]..
- MOLECULAR MECHANISM FOR ERECTILE FUNCTION & DYSFUNCTIONMichael Disanto; Fiscal Year: 2002..It will also provide and explanation for changes in contractility of smooth muscle cells seen in patients with erectile dysfunction. ..
- CYCLIC AMP/ADENOSINE PATHWAYEdwin Jackson; Fiscal Year: 2002..abstract_text> ..
- New Strategies to Enhance Drug Adherence in HypertensionRobert DeBusk; Fiscal Year: 2003..Demonstration of the efficacy of nurse case management of hypertension in the proposed project may facilitate the dissemination of this approach to underserved populations throughout the U.S. ..
- Central betal adrenergic receptors and behaviorHan Ting Zhang; Fiscal Year: 2004..This will lead to the better understanding of pathophysiology and pharmacotherapy of depression. ..
- Role of DEG/ENaC in the renal myogenic responseNIKKI JERNIGAN; Fiscal Year: 2005..abstract_text> ..
- Sertoli Cell Mediated Engulfment of Apoptotic Germ CellsKodi S Ravichandran; Fiscal Year: 2010..abstract_text> ..
- Influences on Sexual HealthMARGAERT NUSBAUM; Fiscal Year: 2007..Nusbaum with experience crucial to her growth as an independent academic researcher in sexual health care. ..
- Neurophysiology and Biomechanics of Urethra in Stress Urinary IncontinenceNaoki Yoshimura; Fiscal Year: 2008..This is recognized as a high priority in the urologic/gynecologic care of SUI patients. [unreadable] [unreadable]..
- Genetic Investigation of Arrhythmogenic Right Ventricular DysplasiaDaniel Judge; Fiscal Year: 2008..A more efficient type of genetic analysis will be tested. This will lead to better understanding of genetic susceptibility to sudden death from heart disease. [unreadable] [unreadable] [unreadable]..
- HU/JHU Head and Neck Cancer Translational Research and *Joseph Califano; Fiscal Year: 2008..unreadable] [unreadable] [unreadable] [unreadable]..
- Prostanoids and hypoxic neonatal pulmonary hypertensionCANDICE FIKE; Fiscal Year: 2009..The goal of this project is to help us understand why infants develop pulmonary hypertension, determine what happens in the lung blood vessels during disease development, and develop treatments for this disease. ..
- AFFERENT PLASTICITY UNDERLYING URETHRAL AND PELVIC PAINNaoki Yoshimura; Fiscal Year: 2010..This is recognized as a high priority in the urologic care of patients with IC/CPPS. ..
- Folate in SchizophreniaDonald C Goff; Fiscal Year: 2010..This will be the first adequately-powered study to assess efficacy and identify predictors of response. ..