Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity
The effect of 17 inhibitors of cyclic nucleotide phosphodiesterases (PDEs) was assayed on cAMP binding activity of Mucor rouxii protein kinase A (PKA), on PKA activity in the absence of cAMP and on free catalytic subunit (C) activity. Isobutylmethylxanthine (IBMX), SQ 20,009 and cilostamide, at 0.2...
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todo:paper_08986568_v5_n5_p615_Tomes2023-10-03T15:44:03Z Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity Tomes, C. Rossi, S. Moreno, S. inhibitors isobutylmethylxanthine Phosphodiesterase protein kinase A 1 ethyl 4 hydrazino 1h pyrazolo[3,4 b]pyridine 5 carboxylic acid ethyl ester 2 amino 4,5 dihydro 6 methyl 5 oxo 4 propyl 1,2,4 triazolo[1,5 a]pyrimidine 4 (3 butoxy 4 methoxybenzyl) 2 imidazolidinone 4,5 dihydro 6 [4 (1h imidazol 1 yl)phenyl] 5 methyl 3(2h) pyridazinone 6 [4 (3 methylureido)phenyl] 3(2h) pyridazinone amrinone cilostamide cilostazol cyclic amp dependent protein kinase dipyridamole etazolate imazodan isobutylmethylxanthine milrinone papaverine phosphodiesterase inhibitor rolipram sq 65442 theophylline unclassified drug article enzyme inhibition ligand binding mucor mucor rouxii nonhuman priority journal signal transduction 1-Methyl-3-isobutylxanthine Animal Cyclic AMP Cyclic AMP-Dependent Protein Kinases Etazolate In Vitro Mucor Myocardium Phosphodiesterase Inhibitors Quinolones Rats Signal Transduction Support, Non-U.S. Gov't Amylomyces rouxii Eukaryota Mucor The effect of 17 inhibitors of cyclic nucleotide phosphodiesterases (PDEs) was assayed on cAMP binding activity of Mucor rouxii protein kinase A (PKA), on PKA activity in the absence of cAMP and on free catalytic subunit (C) activity. Isobutylmethylxanthine (IBMX), SQ 20,009 and cilostamide, at 0.2 mM, behaved as partial agonists of cAMP since they inhibited binding of 0.15 μM [ 3 H]cAMP to the regulatory subunit (R), stimulated slightly PKA activity in the absence of cAMP and did not modify C activity. Amrinone at 0.2 mM inhibited C activity competitively towards ATP. These four compounds displayed the same effects when assayed on eukaryotic protein kinase A types I (PKI) and II (PKII). The combined effect of IBMX and cAMP was analysed on Mucor PKA. Under dissociating conditions (+ 0.5 M NaCl) IBMX antagonized activation by low concentrations of cAMP, while in the absence of NaCl, IBMX potentiated the stimulating activity of cAMP. © 1993. Fil:Tomes, C. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Rossi, S. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Moreno, S. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_08986568_v5_n5_p615_Tomes |
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Universidad de Buenos Aires |
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I-28 |
| repository_str |
R-134 |
| collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
inhibitors isobutylmethylxanthine Phosphodiesterase protein kinase A 1 ethyl 4 hydrazino 1h pyrazolo[3,4 b]pyridine 5 carboxylic acid ethyl ester 2 amino 4,5 dihydro 6 methyl 5 oxo 4 propyl 1,2,4 triazolo[1,5 a]pyrimidine 4 (3 butoxy 4 methoxybenzyl) 2 imidazolidinone 4,5 dihydro 6 [4 (1h imidazol 1 yl)phenyl] 5 methyl 3(2h) pyridazinone 6 [4 (3 methylureido)phenyl] 3(2h) pyridazinone amrinone cilostamide cilostazol cyclic amp dependent protein kinase dipyridamole etazolate imazodan isobutylmethylxanthine milrinone papaverine phosphodiesterase inhibitor rolipram sq 65442 theophylline unclassified drug article enzyme inhibition ligand binding mucor mucor rouxii nonhuman priority journal signal transduction 1-Methyl-3-isobutylxanthine Animal Cyclic AMP Cyclic AMP-Dependent Protein Kinases Etazolate In Vitro Mucor Myocardium Phosphodiesterase Inhibitors Quinolones Rats Signal Transduction Support, Non-U.S. Gov't Amylomyces rouxii Eukaryota Mucor |
| spellingShingle |
inhibitors isobutylmethylxanthine Phosphodiesterase protein kinase A 1 ethyl 4 hydrazino 1h pyrazolo[3,4 b]pyridine 5 carboxylic acid ethyl ester 2 amino 4,5 dihydro 6 methyl 5 oxo 4 propyl 1,2,4 triazolo[1,5 a]pyrimidine 4 (3 butoxy 4 methoxybenzyl) 2 imidazolidinone 4,5 dihydro 6 [4 (1h imidazol 1 yl)phenyl] 5 methyl 3(2h) pyridazinone 6 [4 (3 methylureido)phenyl] 3(2h) pyridazinone amrinone cilostamide cilostazol cyclic amp dependent protein kinase dipyridamole etazolate imazodan isobutylmethylxanthine milrinone papaverine phosphodiesterase inhibitor rolipram sq 65442 theophylline unclassified drug article enzyme inhibition ligand binding mucor mucor rouxii nonhuman priority journal signal transduction 1-Methyl-3-isobutylxanthine Animal Cyclic AMP Cyclic AMP-Dependent Protein Kinases Etazolate In Vitro Mucor Myocardium Phosphodiesterase Inhibitors Quinolones Rats Signal Transduction Support, Non-U.S. Gov't Amylomyces rouxii Eukaryota Mucor Tomes, C. Rossi, S. Moreno, S. Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity |
| topic_facet |
inhibitors isobutylmethylxanthine Phosphodiesterase protein kinase A 1 ethyl 4 hydrazino 1h pyrazolo[3,4 b]pyridine 5 carboxylic acid ethyl ester 2 amino 4,5 dihydro 6 methyl 5 oxo 4 propyl 1,2,4 triazolo[1,5 a]pyrimidine 4 (3 butoxy 4 methoxybenzyl) 2 imidazolidinone 4,5 dihydro 6 [4 (1h imidazol 1 yl)phenyl] 5 methyl 3(2h) pyridazinone 6 [4 (3 methylureido)phenyl] 3(2h) pyridazinone amrinone cilostamide cilostazol cyclic amp dependent protein kinase dipyridamole etazolate imazodan isobutylmethylxanthine milrinone papaverine phosphodiesterase inhibitor rolipram sq 65442 theophylline unclassified drug article enzyme inhibition ligand binding mucor mucor rouxii nonhuman priority journal signal transduction 1-Methyl-3-isobutylxanthine Animal Cyclic AMP Cyclic AMP-Dependent Protein Kinases Etazolate In Vitro Mucor Myocardium Phosphodiesterase Inhibitors Quinolones Rats Signal Transduction Support, Non-U.S. Gov't Amylomyces rouxii Eukaryota Mucor |
| description |
The effect of 17 inhibitors of cyclic nucleotide phosphodiesterases (PDEs) was assayed on cAMP binding activity of Mucor rouxii protein kinase A (PKA), on PKA activity in the absence of cAMP and on free catalytic subunit (C) activity. Isobutylmethylxanthine (IBMX), SQ 20,009 and cilostamide, at 0.2 mM, behaved as partial agonists of cAMP since they inhibited binding of 0.15 μM [ 3 H]cAMP to the regulatory subunit (R), stimulated slightly PKA activity in the absence of cAMP and did not modify C activity. Amrinone at 0.2 mM inhibited C activity competitively towards ATP. These four compounds displayed the same effects when assayed on eukaryotic protein kinase A types I (PKI) and II (PKII). The combined effect of IBMX and cAMP was analysed on Mucor PKA. Under dissociating conditions (+ 0.5 M NaCl) IBMX antagonized activation by low concentrations of cAMP, while in the absence of NaCl, IBMX potentiated the stimulating activity of cAMP. © 1993. |
| format |
JOUR |
| author |
Tomes, C. Rossi, S. Moreno, S. |
| author_facet |
Tomes, C. Rossi, S. Moreno, S. |
| author_sort |
Tomes, C. |
| title |
Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity |
| title_short |
Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity |
| title_full |
Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity |
| title_fullStr |
Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity |
| title_full_unstemmed |
Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity |
| title_sort |
isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect camp-dependent protein kinase activity |
| url |
http://hdl.handle.net/20.500.12110/paper_08986568_v5_n5_p615_Tomes |
| work_keys_str_mv |
AT tomesc isobutylmethylxanthineandotherclassicalcyclicnucleotidephosphodiesteraseinhibitorsaffectcampdependentproteinkinaseactivity AT rossis isobutylmethylxanthineandotherclassicalcyclicnucleotidephosphodiesteraseinhibitorsaffectcampdependentproteinkinaseactivity AT morenos isobutylmethylxanthineandotherclassicalcyclicnucleotidephosphodiesteraseinhibitorsaffectcampdependentproteinkinaseactivity |
| _version_ |
1807320330203561984 |