| http://purl.uniprot.org/citations/15878705 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/15878705 | http://www.w3.org/2000/01/rdf-schema#comment | "We used antagonists of cGMP-phosphodiesterases to examine the role of cGMP for light-scattering oscillations and cAMP-induced Ca(2+)-influx in Dictyostelium discoideum, however, SCH 51866 (cis-5,6a,7,8,9,9a-hexahydro-2-[4-(trifluoromethyl)phenylmethyl]-5-methyl-cyclopent[4,5]imidazo[2,1-b]purin-4(3H)-one) and sildenafil citrate (1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1-H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine citrate) were poor inhibitors of cGMP-hydrolysis. Instead, SCH 51866 (IC(50) = 16 microM) and sildenafil, blocked chemoattractant (cAMP)-induced Ca(2+)-influx as determined with a Ca(2+)-specific electrode. SCH 51866 (150 microM) affected neither spontaneous cGMP transients during light-scattering-oscillations nor cAMP-mediated K(+)-efflux. SCH 51866 and sildenafil are competitive inhibitors of cGMP phosphodiesterases. However, the activity of cGMP-dependent protein kinase Ialpha (PKGIalpha) was not altered by SCH 51866 (150 microM). By contrast, patch-clamp measurements of bovine cone cGMP-gated-channels (cyclic-nucleotide-gated-channel, CNGA3), stably expressed in human embryonic kidney cells, HEK 293 cells, revealed reversible, competitive and dose-dependent inhibition of sodium currents by SCH 51866 (IC(50) = 25 microM) and sildenafil, but not by another inhibitor of cGMP-phosphodiesterases, UK 114,542. The possibility that D. discoideum cells also express a cGMP-regulated channel is supported by our finding that LY 83583 (6-(phenylamino)-5,8-quinolinedione) (35 microM), known to inhibit cyclic-nucleotide-gated-channels as well as guanylyl-cyclases, reduced cAMP-induced Ca(2+)-influx in D. discoideum, but did not affect cAMP-induced cGMP accumulation. Utilizing a PDED null strain that exhibits a prolonged and elevated cGMP transient following receptor activation, we found that the inhibition of Ca(2+)-influx by SCH 51866 in the wildtype was absent in the mutant. Our results show that SCH 51866 and sildenafil are antagonists of a Ca(2+)-permeable channel (CNGA3) and that both compete with cGMP for a regulatory site of Ca(2+)-influx in D. discoideum."xsd:string |
| http://purl.uniprot.org/citations/15878705 | http://purl.org/dc/terms/identifier | "doi:10.1016/j.ejphar.2005.01.047"xsd:string |
| http://purl.uniprot.org/citations/15878705 | http://purl.uniprot.org/core/author | "Lusche D.F."xsd:string |
| http://purl.uniprot.org/citations/15878705 | http://purl.uniprot.org/core/author | "Malchow D."xsd:string |
| http://purl.uniprot.org/citations/15878705 | http://purl.uniprot.org/core/author | "Kaneko H."xsd:string |
| http://purl.uniprot.org/citations/15878705 | http://purl.uniprot.org/core/date | "2005"xsd:gYear |
| http://purl.uniprot.org/citations/15878705 | http://purl.uniprot.org/core/name | "Eur J Pharmacol"xsd:string |
| http://purl.uniprot.org/citations/15878705 | http://purl.uniprot.org/core/pages | "9-20"xsd:string |
| http://purl.uniprot.org/citations/15878705 | http://purl.uniprot.org/core/title | "cGMP-phosphodiesterase antagonists inhibit Ca2+-influx in Dictyostelium discoideum and bovine cyclic-nucleotide-gated-channel."xsd:string |
| http://purl.uniprot.org/citations/15878705 | http://purl.uniprot.org/core/volume | "513"xsd:string |
| http://purl.uniprot.org/citations/15878705 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/15878705 |
| http://purl.uniprot.org/citations/15878705 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/15878705 |
| http://purl.uniprot.org/uniprot/#_B0G0Y8-mappedCitation-15878705 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/15878705 |
| http://purl.uniprot.org/uniprot/#_P12019-mappedCitation-15878705 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/15878705 |
| http://purl.uniprot.org/uniprot/#_Q8MLZ3-mappedCitation-15878705 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/15878705 |
| http://purl.uniprot.org/uniprot/#_Q8MM62-mappedCitation-15878705 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/15878705 |
| http://purl.uniprot.org/uniprot/Q8MLZ3 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/15878705 |
| http://purl.uniprot.org/uniprot/P12019 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/15878705 |
| http://purl.uniprot.org/uniprot/B0G0Y8 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/15878705 |
| http://purl.uniprot.org/uniprot/Q8MM62 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/15878705 |