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Abstract:

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.

Registro:

Documento: Artículo
Título:Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity
Autor:Tomes, C.; Rossi, S.; Moreno, S.
Filiación:Departamento de Química Biológica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, 1428 Buenos Aires, Argentina
Palabras clave: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
Año:1993
Volumen:5
Número:5
Página de inicio:615
Página de fin:621
DOI: http://dx.doi.org/10.1016/0898-6568(93)90056-R
Título revista:Cellular Signalling
Título revista abreviado:Cell. Signal.
ISSN:08986568
CODEN:CESIE
CAS:1-Methyl-3-isobutylxanthine, 28822-58-4; cilostamide, 68550-75-4; Cyclic AMP, 60-92-4; Cyclic AMP-Dependent Protein Kinases, EC 2.7.1.37; Etazolate, 51022-77-6; Phosphodiesterase Inhibitors; Quinolones
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_08986568_v5_n5_p615_Tomes

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Citas:

---------- APA ----------
Tomes, C., Rossi, S. & Moreno, S. (1993) . Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity. Cellular Signalling, 5(5), 615-621.
http://dx.doi.org/10.1016/0898-6568(93)90056-R
---------- CHICAGO ----------
Tomes, C., Rossi, S., Moreno, S. "Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity" . Cellular Signalling 5, no. 5 (1993) : 615-621.
http://dx.doi.org/10.1016/0898-6568(93)90056-R
---------- MLA ----------
Tomes, C., Rossi, S., Moreno, S. "Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity" . Cellular Signalling, vol. 5, no. 5, 1993, pp. 615-621.
http://dx.doi.org/10.1016/0898-6568(93)90056-R
---------- VANCOUVER ----------
Tomes, C., Rossi, S., Moreno, S. Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity. Cell. Signal. 1993;5(5):615-621.
http://dx.doi.org/10.1016/0898-6568(93)90056-R