2-Aminopurine inhibits the double-stranded RNA-dependent protein kinase both in vitro and in vivo. 1993

Y Hu, and T W Conway
Department of Biochemistry, University of Iowa, Iowa City 52242.

The autophosphorylation of interferon (IFN)-induced double-stranded RNA-dependent p68 protein kinase (PKR) and phosphorylation of the alpha-subunit of the translation initiation factor eIF-2 were inhibited by 10 mM 2-aminopurine in vitro. High concentrations of ATP overcame the inhibition. Kinetic studies indicated that 2-aminopurine is a competitive inhibitor with respect to ATP, suggesting that these two molecules bind the same site on the kinase. Treatment of HeLa cells with poly(I):poly(C) stimulated PKR autophosphorylation in vivo. The stimulated activity was inhibited by 10 mM 2-aminopurine to approximately the same extent as the in vitro inhibition.

UI MeSH Term Description Entries
D010766 Phosphorylation The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety. Phosphorylations
D004789 Enzyme Activation Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme. Activation, Enzyme,Activations, Enzyme,Enzyme Activations
D006367 HeLa Cells The first continuously cultured human malignant CELL LINE, derived from the cervical carcinoma of Henrietta Lacks. These cells are used for, among other things, VIRUS CULTIVATION and PRECLINICAL DRUG EVALUATION assays. Cell, HeLa,Cells, HeLa,HeLa Cell
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000255 Adenosine Triphosphate An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter. ATP,Adenosine Triphosphate, Calcium Salt,Adenosine Triphosphate, Chromium Salt,Adenosine Triphosphate, Magnesium Salt,Adenosine Triphosphate, Manganese Salt,Adenylpyrophosphate,CaATP,CrATP,Manganese Adenosine Triphosphate,MgATP,MnATP,ATP-MgCl2,Adenosine Triphosphate, Chromium Ammonium Salt,Adenosine Triphosphate, Magnesium Chloride,Atriphos,Chromium Adenosine Triphosphate,Cr(H2O)4 ATP,Magnesium Adenosine Triphosphate,Striadyne,ATP MgCl2
D015075 2-Aminopurine A purine that is an isomer of ADENINE (6-aminopurine). 2 Aminopurine
D017346 Protein Serine-Threonine Kinases A group of enzymes that catalyzes the phosphorylation of serine or threonine residues in proteins, with ATP or other nucleotides as phosphate donors. Protein-Serine-Threonine Kinases,Serine-Threonine Protein Kinase,Serine-Threonine Protein Kinases,Protein-Serine Kinase,Protein-Serine-Threonine Kinase,Protein-Threonine Kinase,Serine Kinase,Serine-Threonine Kinase,Serine-Threonine Kinases,Threonine Kinase,Kinase, Protein-Serine,Kinase, Protein-Serine-Threonine,Kinase, Protein-Threonine,Kinase, Serine-Threonine,Kinases, Protein Serine-Threonine,Kinases, Protein-Serine-Threonine,Kinases, Serine-Threonine,Protein Kinase, Serine-Threonine,Protein Kinases, Serine-Threonine,Protein Serine Kinase,Protein Serine Threonine Kinase,Protein Serine Threonine Kinases,Protein Threonine Kinase,Serine Threonine Kinase,Serine Threonine Kinases,Serine Threonine Protein Kinase,Serine Threonine Protein Kinases
D019892 eIF-2 Kinase A dsRNA-activated cAMP-independent protein serine/threonine kinase that is induced by interferon. In the presence of dsRNA and ATP, the kinase autophosphorylates on several serine and threonine residues. The phosphorylated enzyme catalyzes the phosphorylation of the alpha subunit of EUKARYOTIC INITIATION FACTOR-2, leading to the inhibition of protein synthesis. Protein Kinase PKR,Protein Kinase, RNA Activated,RNA-Dependent Protein Kinase,p68 Kinase,DAI Protein Kinase,DSRNA-Dep Protein Kinase,Double Stranded RNA-Dependent Kinase (dsl),Double Stranded RNA-Dependent eIF-2 alpha Protein Kinase,Eukaryotic Initiation Factor 2alpha Kinase,Heme Controlled Repressor,Heme-Controlled Inhibitor,Heme-Controlled Translational Repressor,Heme-Regulated eIF-2alpha Kinase,Hemin Controlled Repressor,Hemin-Controlled Translational Repressor,P68 Protein Kinase,Self-Phosphorylating Protein Kinase,TIK Kinase,dsRNA-Activated Inhibitor,eIF-2alpha Kinase,eRF, eIF-2 Recycling Factor,p65 Kinase,Controlled Repressor, Heme,Controlled Repressor, Hemin,DSRNA Dep Protein Kinase,Double Stranded RNA Dependent eIF 2 alpha Protein Kinase,Heme Controlled Inhibitor,Heme Controlled Translational Repressor,Heme Regulated eIF 2alpha Kinase,Hemin Controlled Translational Repressor,Inhibitor, Heme-Controlled,Inhibitor, dsRNA-Activated,Kinase PKR, Protein,Kinase, DAI Protein,Kinase, DSRNA-Dep Protein,Kinase, Heme-Regulated eIF-2alpha,Kinase, P68 Protein,Kinase, RNA-Dependent Protein,Kinase, Self-Phosphorylating Protein,Kinase, TIK,Kinase, eIF-2,Kinase, eIF-2alpha,Kinase, p65,Kinase, p68,PKR, Protein Kinase,Protein Kinase, DAI,Protein Kinase, DSRNA-Dep,Protein Kinase, P68,Protein Kinase, RNA-Dependent,Protein Kinase, Self-Phosphorylating,RNA Dependent Protein Kinase,Repressor, Heme Controlled,Repressor, Heme-Controlled Translational,Repressor, Hemin Controlled,Repressor, Hemin-Controlled Translational,Self Phosphorylating Protein Kinase,Translational Repressor, Heme-Controlled,Translational Repressor, Hemin-Controlled,dsRNA Activated Inhibitor,eIF 2 Kinase,eIF 2alpha Kinase,eIF-2alpha Kinase, Heme-Regulated,eRF, eIF 2 Recycling Factor
D066298 In Vitro Techniques Methods to study reactions or processes taking place in an artificial environment outside the living organism. In Vitro Test,In Vitro Testing,In Vitro Tests,In Vitro as Topic,In Vitro,In Vitro Technique,In Vitro Testings,Technique, In Vitro,Techniques, In Vitro,Test, In Vitro,Testing, In Vitro,Testings, In Vitro,Tests, In Vitro,Vitro Testing, In

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