Irreversible inhibition of adenylate cyclase by 5'-(p-bromomethylbenzoyl) adenosine.
The effect of 5'-(p-bromomethylbenzoyl) adenosine (pBMBA) on adenylate cyclase from bovine caudate nucleus membranes was studied. Adenylyl-5'-methylenediphosphonate (but not adenosine) protected adenylate cyclase against inactivation by this compound. The degree of pBMBA-induced inhibition of adenylate cyclase increased in the presence of Mg2+. 5'-(p-fluorosulfonylbenzoyl) adenosine (pFSBA) was also a specific irreversible inhibitor of adenylate cyclase. It was demonstrated that the enzyme inactivated by pFSBA completely restored its activity under the action of dithiothreitol. The results obtained are indicative of the presence of the -SH group in the enzyme active site.
D000241:Adenosine / Q000031:analogs & derivatives* / Q000494:pharmacology; D000255:Adenosine Triphosphate / Q000031:analogs & derivatives / Q000494:pharmacology; D000067956:Adenylyl Cyclase Inhibitors; D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D002417:Cattle; D002421:Caudate Nucleus / Q000201:enzymology*; D002462:Cell Membrane / Q000201:enzymology; D004229:Dithiothreitol / Q000494:pharmacology; D007700:Kinetics
D000067956:Adenylyl Cyclase Inhibitors; C005147:5'-adenylyl (beta,gamma-methylene)diphosphonate; C010959:5'-(4-fluorosulfonylbenzoyl)adenosine; D000255:Adenosine Triphosphate; C046041:5'-(4-bromomethylbenzoyl)adenosine; D000241:Adenosine; C002630:alpha,beta-methyleneadenosine 5'-triphosphate; D004229:Dithiothreitol