Inhibition of protein kinase activity of phorboid and ingenoid receptor by di(adenosine-5')oligophosphate.
Di(adenosine-5')oligophosphate nucleotides of general structure ApnA (n = 3-6) inhibited the protein kinase activity of homogeneous phorboid receptor. These nucleotides did not affect the phorboid binding activity. Ap4A competed for an ATP binding site on the phorboid receptor. Km for ATP was increased from 0.5 to 2 microM in the presence of 0.2 mM of Ap4A. KI was calculated to be approximately 0.1 mM. Ap4A-elicited inhibition of phorboid receptor kinase activity was independent of receptor concentration as well as of phosphoacceptor substrate concentration.
D000227:Adenine Nucleotides / Q000494:pharmacology*; D000255:Adenosine Triphosphate / Q000494:pharmacology; D000818:Animals; D001921:Brain / Q000378:metabolism; D029742:Caenorhabditis elegans Proteins; D002352:Carrier Proteins; D006657:Histones / Q000494:pharmacology; D066298:In Vitro Techniques; D051379:Mice; D015240:Phorbol 12,13-Dibutyrate; D010703:Phorbol Esters / Q000378:metabolism; D011493:Protein Kinase C; D047428:Protein Kinase Inhibitors; D011955:Receptors, Drug / Q000187:drug effects / Q000378:metabolism*; D011971:Receptors, Immunologic / Q000187:drug effects / Q000378:metabolism*
D000227:Adenine Nucleotides; D029742:Caenorhabditis elegans Proteins; D002352:Carrier Proteins; D006657:Histones; D010703:Phorbol Esters; D047428:Protein Kinase Inhibitors; D011955:Receptors, Drug; D011971:Receptors, Immunologic; C027777:ingenol ester receptor; C083141:phorbol ester binding protein; C027776:phorbol ester receptor; D015240:Phorbol 12,13-Dibutyrate; D000255:Adenosine Triphosphate; D011493:Protein Kinase C