Recombinant Human cGMP-specific 3',5'-cyclic phosphodiesterase (PDE5A), partial

1. Thsese findings provide insight into the existence of distinct "pools" of PDE5A in human arterial smooth muscle cells and support the idea that these discrete compartments regulate distinct cGMP-dependent events. PMID: 28506928
2. The analogues showed a relative narrow range of Ki values for PDE5A inhibition (1.2-14 nm). PMID: 28211580
3. Data indicate that high type 5 phosphodiesterase (PDE5) expression in glioblastoma multiforme (GBM) cells significantly correlated with longer overall survival of patients. PMID: 28099939
4. the relationship between PDE5A polymorphisms, diabetes, and the efficacy of sildenafil treatment.The response to sildenafil treatment depends on polymorphisms in the PDE5A gene and the glycemic status of the patients. PMID: 27235284
5. Study showed that past attempts to quantify PDE5 mRNA were flawed due to the use of incorrect primers, and that when correct primers are used, PDE5 mRNA is detectable in human brain tissue; that PDE5 protein exists in human brain by western blot and ELISA; and performed immunohistochemistry and demonstrate that PDE5 is present in human neurons. PMID: 26967220
6. Our data showed a significant and previously undocumented upregulation of PDE5 in both rat and human BPH. PMID: 26657792
7. Overexpression of PDE5 in papillary thyroid carcinomas. PMID: 25837309
8. cGMP PDE isozymes, PDE5 and 10, are elevated in colon tumor cells compared with normal colonocytes, and inhibitors and siRNAs can selectively suppress colon tumor cell growth PMID: 26299804
9. Results show that Ser102 and Ser104 may influence the conformational flexibility of PDE5A, which may in turn influence phosphorylation status, allosteric regulation by cGMP or other as yet unknown regulatory mechanisms for PDE5A. PMID: 25247292
10. PDE5A appears to jointly influence amygdala volume and emotion recognition performance. PMID: 25322361
11. inhibition of PDE5 can counteract apoptosis during aging by modulating proand antiapoptotic molecules and the APP pathway. PMID: 24112792
12. Myocardial PDE5 expression is increased in the hearts of humans and mice with chronic pressure overload. PMID: 23527037
13. it is concluded that assessment of PDE5 and PDE9 expression may be useful in the differential diagnosis of benign and malignant breast disease and successful treatment of breast cancer PMID: 22960860
14. analysis of amino acid residues responsible for the selectivity of tadalafil binding to two closely related phosphodiesterases, PDE5 and PDE6 PMID: 23033484
15. 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 PMID: 22843873
16. 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. PMID: 21736695
17. 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. PMID: 21987443
18. found in smooth muscle wall of blood vessels transversing the clitoral supepithelial and stromal space PMID: 21697861
19. the spatial localization of PDE5A at the level of caveolin-rich lipid rafts allows for a feedback loop between endothelial PDE5A and nitric oxide synthase (NOS3) PMID: 21421555
20. These studies suggest a novel role for PDE5 in erythrocytes. PMID: 21525805
21. Solved is the crystal structure of the structurally uncharacterized PDE5A GAF-B domain. PMID: 21425347
22. The distribution of PDE-5 and NOD II may indicate a physiologic role in the regulatory function of human vagina. PMID: 20177899
23. Distinct allostery induced in the cyclic GMP-binding, cyclic GMP-specific phosphodiesterase (PDE5) by cyclic GMP, sildenafil, and metal ions. PMID: 21193396
24. In melanoma cells, oncogenic (V600E) BRAF signaling downregulates PDE5A through the transcription factor BRN2, leading to increased cGMP and Ca2+ and the induction of invasion through increased cell contractility. PMID: 21215707
25. Conformation changes, N-terminal involvement, and cGMP signal relay in the phosphodiesterase-5 GAF domain. PMID: 20861010
26. PDE5-inhibition blocks TRPC6 channel activation and associated Cn/NFAT activation signaling by PKG-dependent channel phosphorylation PMID: 19961855
27. Suggest that PDE5A is associated with increased disease susceptibility, pathological progression, and development of proteinuria in childhood IgA nephropathy. PMID: 20563733
28. The rAd5-shRNA-PDE5A3 can obviously increase the cGMP level in the smooth muscle cells of human corpus cavernosum, and enhance the inhibition of the PDE5 gene. PMID: 19852267
29. Data show that the identified compound will be a useful agent for evaluating the therapeutic potential of central inhibition of PDE5. PMID: 20196613
30. High PDE5A1 expression is associated with malignant melanoma. PMID: 20332439
31. Myocardial oxidative stress increases PDE5 expression in the failing heart PMID: 20308615
32. Data show that SS increased intracellular cGMP levels and activated protein kinase G, and selectively inhibited PDE5 in breast tumor cells. PMID: 19996273
33. Human PDE5A gene encodes three PDE5 isoforms from two alternate promoters. PMID: 11896473
34. cGMP-directed regulation of PDE5 phosphorylation and the resulting increase in cGMP binding affinity occur largely within the R domain PMID: 12359732
35. CGMP-dependent protein kinase I causes NO-induced PDE5 phosphorylation. However, cGMP can directly activate PDE5 without phosphorylation in platelet cytosol, most likely by binding to GAF domains. PMID: 12604588
36. GAFa domain of PDE5A adopts a structure similar to the GAFb domain of PDE2A, and provides the sole site for cGMP binding in PDE5A PMID: 12650945
37. 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) PMID: 12955149
38. Crystal structures of phosphodiesterases 4 and 5 in complex with inhibitor 3-isobutyl-1-methylxanthine PMID: 14668322
39. demonstrated, for the first time, that androgens positively regulate phosphodiesterase 5 PMID: 14764637
40. no correlations of a novel polymorphism of the PDE5A promoter gene with the intermediate phenotype essential hypertension/erectile dysfunction PMID: 15175637
41. Phosphorylation of PDE5 seems to act as memory switch for activation leading to long-term desensitization of the signaling pathway. PMID: 15240816
42. PDE5 gene expression and activity are androgen-dependent in vas deferens. PMID: 15640438
43. Phosphodiesterase Type 5 is the main factor regulating cyclic guanosine monophosphate hydrolysis and downstream signaling in human PASMCs. PMID: 15817798
44. Results suggest that glutamine(817) is a positive determinant for phosphodiesterase 5 affinity for cyclic GMP and several inhibitors. PMID: 16407275
45. Subdomains are structurally and functionally interdependent and act in concert in regulating human PDE5. PMID: 16690614
46. Virtually all tissues and cell types express PDE5, with heart and cardiomyocytes being contentious; PDE5A1 and PDE5A2 are ubiquitous, but PDE5A3 is specific to smooth muscle, as described in this review. PMID: 17017938
47. PDE5 may be a possible therapeutic target in bladder dysfunction for ameliorating irritative lower urinary tract symptoms. PMID: 17138653
48. The PDE-5A was expressed in both pre-adipocytes and adipocytes. PDE-5A mRNA and protein levels decreased as pre-adipocytes differentiated. PMID: 17906676
49. GAF domains of PDE5A can act as sensors and intracellular sinks for cyclic GMP, but not cyclic AMP. PMID: 18293931
50. analysis of functional chimeras of the phosphodiesterase 5 and 10 tandem GAF domains PMID: 18635550

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HGNC: 8784

OMIM: 603310

KEGG: hsa:8654

STRING: 9606.ENSP00000347046

UniGene: Hs.647971