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Phosphodiesterase 5A, cGMP-specific

This gene encodes a cGMP-binding, cGMP-specific phosphodiesterase, a member of the cyclic nucleotide phosphodiesterase family. This phosphodiesterase specifically hydrolyzes cGMP to 5'-GMP. It is involved in the regulation of intracellular concentrations of cyclic nucleotides and is important for smooth muscle relaxation in the cardiovascular system. Alternative splicing of this gene results in three transcript variants encoding distinct isoforms. [provided by RefSeq, Jul 2008] (from NCBI)
Top mentioned proteins: Phosphodiesterase, PDE, CAN, MEN, HAD
Papers on PDE5
Dose-Dependent Effects of Glucocorticoids on Pulmonary Vascular Development in a Murine Model of Hyperoxic Lung Injury.
Farrow et al., Chicago, United States. In Pediatr Res, Feb 2016
BACKGROUND: Exposure of neonatal mice to hyperoxia results in pulmonary vascular remodeling and aberrant phosphodiesterase-5 (PDE5) signaling.
Roles of phosphodiesterases in the regulation of the cardiac cyclic nucleotide cross-talk signaling network.
Winslow et al., Baltimore, United States. In J Mol Cell Cardiol, Feb 2016
Finally, we show that PDE2 compensates for inhibition of PDE5 both in terms of cGMP and cAMP dynamics, leading to cGMP elevation and increased PKG activation, while maintaining whole-cell β-adrenergic responses similar to that prior to PDE5 inhibition.
The efficacy of udenafil in end-stage renal disease patients undergoing hemodialysis.
Atilla et al., Samsun, Turkey. In Ren Fail, Feb 2016
Different phosphodiesterase type 5 (PDE-5) inhibitors have been used, and efficacies revealed, for the treatment of ED in HD patients; however, there are no studies related to udenafil use or results for HD patients.
Novel Therapeutic Targets for Phosphodiesterase 5 Inhibitors: current state-of-the-art on systemic arterial hypertension and atherosclerosis.
Meyrelles et al., Vila Velha, Brazil. In Curr Pharm Biotechnol, Jan 2016
UNASSIGNED: The usefulness of selective inhibitors of phosphodiesterase 5 (PDE5) is well known, first for the treatment of male erectile dysfunction and more recently for pulmonary hypertension.
[Second and third-lines therapy for the management of erectile dysfunction].
Vaucher et al., In Rev Med Suisse, Jan 2016
Second-line strategies can also be considered upfront in patients with contraindications to PDE5 inhibitors.
Clinical and preclinical treatment of urologic diseases with phosphodiesterase isoenzymes 5 inhibitors: an update.
Zhang et al., Wuhan, China. In Asian J Androl, Dec 2015
UNASSIGNED: Phosphodiesterase isoenzymes 5 inhibitors (PDE5-Is) are the first-line therapy for erectile dysfunction (ED).
Use of Phosphodiesterase Type 5 Inhibitors for Erectile Dysfunction and Risk of Malignant Melanoma.
Stattin et al., Uppsala, Sweden. In Jama, Jul 2015
IMPORTANCE: The target for the oral erectile dysfunction drugs, phosphodiesterase type 5 (PDE5) inhibitors, is part of a pathway implicated in the development of malignant melanoma.
Sildenafil does not enhance but rather attenuates vasorelaxant effects of antidiabetic agents.
Phelps et al., In J Smooth Muscle Res, 2014
Type 2 diabetic men commonly experience erectile dysfunction for which phosphodiesterase-5 (PDE5) inhibitors like sildenafil (Viagra) are often recommended.
The limits of oral therapy in pulmonary arterial hypertension management.
Jing et al., Shanghai, China. In Ther Clin Risk Manag, 2014
Over the past decade, new treatments for PAH, such as the use of ERAs, PDE-5 inhibitors and prostacyclin analogs, have brought about dramatic improvements in clinical outcomes.
Novel Therapeutic Strategies for Reducing Right Heart Failure Associated Mortality in Fibrotic Lung Diseases.
Oyenuga et al., Chicago, United States. In Biomed Res Int, 2014
Specific therapies targeting pulmonary hypertension include calcium channel blockers, endothelin (ET-1) receptor antagonists, prostacyclin analogs, phosphodiesterase type 5 (PDE5) inhibitors, and rho-kinase (ROCK) inhibitors.
Phosphodiesterase-5 Inhibitors: Action on the Signaling Pathways of Neuroinflammation, Neurodegeneration, and Cognition.
Garcia-Osta et al., Recife, Brazil. In Mediators Inflamm, 2014
Phosphodiesterase type 5 inhibitors (PDE5-Is) have recently emerged as a potential therapeutic strategy for neuroinflammatory, neurodegenerative, and memory loss diseases.
Sildenafil reduces respiratory muscle weakness and fibrosis in the mdx mouse model of Duchenne muscular dystrophy.
Froehner et al., Seattle, United States. In J Pathol, 2012
Sildenafil-mediated PDE5 inhibition significantly reduces diaphragm respiratory muscle dysfunction and pathology in the mdx mouse model of Duchenne muscular dystrophy.
Pathological cardiac hypertrophy alters intracellular targeting of phosphodiesterase type 5 from nitric oxide synthase-3 to natriuretic peptide signaling.
Kass et al., Baltimore, United States. In Circulation, 2012
PDE5 inhibition did not alter atrial natriuretic peptide-stimulated cGMP in the resting heart but augmented it in the transaortic constriction heart.
Increased gene expression of the ABCC5 transporter without distinct changes in the expression of PDE5 in human cervical cancer cells during growth.
Ørbo et al., Tromsø, Norway. In Anticancer Res, 2012
PDE5 is highly expressed and increases ( approximately 130%) during growth whereas ABCC5 exhibited low to moderate expression, with a moderate increase ( approximately 40%) during growth
Phosphodiesterase type 9 (PDE9) in the human lower urinary tract: an immunohistochemical study.
Sasano et al., Sendai, Japan. In Bju Int, 2012
PDE9 is widely distributed in the urothelial epithelium of the human lower urinary tract and its potential roles may be different from those of PDE5.
t(4;8)(q27;q24) in Hodgkin lymphoma cells targets phosphodiesterase PDE5A and homeobox gene ZHX2.
MacLeod et al., Braunschweig, Germany. In Genes Chromosomes Cancer, 2011
Treatment of L-1236 with PDE5A-inhibitor sildenafil or with siRNA directed against PDE5A and concomitant stimulation with cyclic guanosine monophosphate (cGMP) resulted in enhanced apoptosis, indicating PDE5A as an oncogene.
cGMP-dependent protein kinases and cGMP phosphodiesterases in nitric oxide and cGMP action.
Sibley et al., Nashville, United States. In Pharmacol Rev, 2010
Current therapies that have successfully targeted the NO-signaling pathway include nitrovasodilators (nitroglycerin), PDE5 inhibitors [sildenafil (Viagra and Revatio), vardenafil (Levitra), and tadalafil (Cialis and Adcirca)] for treatment of a number of vascular diseases including angina pectoris, erectile dysfunction, and pulmonary hypertension; the PDE3 inhibitors [cilostazol (Pletal) and milrinone (Primacor)] are used for treatment of intermittent claudication and acute heart failure, respectively.
Phase I and II study of exisulind in combination with capecitabine in patients with metastatic breast cancer.
Hortobagyi et al., Houston, United States. In J Clin Oncol, 2003
Fourteen specimens were available for immunohistochemical assessment of phosphodiesterase-5 isoenzyme (PDE-5) and PDE-2 expression, which are the targets of exisulind.
Structure of the catalytic domain of human phosphodiesterase 5 with bound drug molecules.
Cho et al., Taejŏn, South Korea. In Nature, 2003
three-dimensional structures of the catalytic domain (residues 537-860) of human PDE5 complexed with the three drug molecules sildenafil, tadalafil (Cialis) and vardenafil (Levitra)
Phosphodiesterase 5 inhibitors: current status and potential applications.
Rotella, Princeton, United States. In Nat Rev Drug Discov, 2002
Phosphodiesterase 5 (PDE5) inhibition is now a widely accepted and efficacious therapeutic option for the treatment of erectile dysfunction in men, as a result of extensive clinical experience with sildenafil and other new PDE5 inhibitors.
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