2',5'-Dideoxyadenosine 3'-polyphosphates are potent inhibitors of adenylyl cyclases.
2',5'-Dideoxyadenosine 3'-di- and triphosphates were tested as inhibitors of brain adenylyl cyclases. With an IC50 approximately 40 nM, 2',5'-dideoxy-3'-ATP is the most potent nonprotein synthetic regulator of adenylyl cyclases thus far described. Neither 2',5'-dideoxy-3'-ADP nor 2',5'-dideoxy-3'-ATP inhibited activity by competition with substrate, and the linear noncompetitive inhibition observed was consistent with interaction via a distinct domain. The availability of this ligand will permit the development of a variety of probes that will be extremely useful in investigating adenylyl cyclase structure and the role(s) that this class of compound may play in physiologically regulating cell function.
Désaubry
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L
Department of Physiology and Biophysics, State University of New York, Stony Brook 11794-8661, USA.
Shoshani
I
I
Johnson
R A
RA
D000067956:Adenylyl Cyclase Inhibitors; D000818:Animals; D001921:Brain / Q000201:enzymology; D002417:Cattle; D003838:Deoxyadenine Nucleotides / Q000494:pharmacology*; D054306:Dideoxynucleotides; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D051381:Rats
D000067956:Adenylyl Cyclase Inhibitors; D003838:Deoxyadenine Nucleotides; D054306:Dideoxynucleotides; D004791:Enzyme Inhibitors; C037773:2',3'-dideoxyadenosine triphosphate