Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.4.1 (phosphodiesterase)
 18,767 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A series of triesters of adenosine cyclic 3',5'-phosphate was synthesized by treatment of the free acid with various diazoalkanes (R=H, CH3, C6H5,0-NO2C6H4, p-NO2C6H4, p-CH3C6H4). The resulting diastereomeric mixtures were separated into their axial and equatorial components. Hydrolysis of the compounds was examined as well as photolysis of the photolabile o-nitrobenzyl ester. All compounds were then tested for their ability to activate the cAMP-dependent protein kinase and for their ability to serve as a substrate for the cAMP phosphodiesterase showing almost no effect on either enzyme. In a biological assay the benzyl triesters were able to penetrate into C 6 rat glioma cells and to induce the typical morphological alteration of the cell shape known for high cellular levels of cAMP. It was concluded that the benzyl triesters of cAMP are useful derivatives which can be efficiently and specifically converted to the parent nucleotide. Benzyl derivatives of biologically active phosphodiesters may provide a useful tool for study in biology and pharmacology.
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PMID:Synthesis, structure, and reactivity of adenosine cyclic 3',5'-phosphate benzyl triesters. 19 57

Rat C 6 glioma is known to possess a beta-adrenergic receptor with which intracellular cyclic adenosine monophosphate (cAMP) levels are altered to control cell growth in vitro. In order to study the effect of beta-adrenergic agonist, isoproterenol, in growth-inhibitory action upon C 6 glioma cells, subcutaneous tumor models and meningeal gliomatisis (MG) models as a brain tumor model have been exposed to the treatment of isoproterenol. Growth of subcutaneous tumor was suppressed by the treatment of the drug, and the survival time of MG rats was prolonged by the intrathecal (i. t.) injection of isoproterenol. The addition of papaverine, phosphodiesterase inhibitor, to the treatment schedule augmented the growth-inhibitory effect of isoproterenol. Therefore, it is concluded that the survival time of the brain tumor models could be prolonged through the inhibition of the growth of C 6 glioma cells by such drugs as those which elevate intracellular cAMP levels.
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PMID:[Treatment of rat glioma with a beta-adrenergic agonist and a phosphodiesterase inhibitor in vivo]. 282 9