A preparation of galactosyl ceramide galactosidase from rat brain has been tested with potential inhibitors which resemble the enzyme’s substrate. The amide made from 2-hydroxydodecanoic acid and nL-erythro-3-phenyl-2-amino-1,3-propanediol proved to be a fine inhibitor, acting noncompetitively. Removal of any of the three hydroxyl groups reduced the effectiveness, as did inversion of the C-3 ca...

Different inhibition types of the saturation kinetics involving a synthesized model complex, [Bu4N]3[MoVIO2(mnt)2] (E) (where mnt2- = 1,2-dicyanoethylenedithiolate), and HSO3- as the substrate (S) by structurally similar anions SO4(2-), H2PO4- and H2PO3- have been shown for the first time in relevance to the reductive half reaction of the native enzyme sulphite oxidase. SO4(2-) acts as a compet...

The kinase Akt plays a central role as a regulator of multiple growth factor input signals, thus making it an attractive anticancer drug target. A-443654 is an ATP-competitive Akt inhibitor. Unexpectedly, treatment of cells with A-443654 causes paradoxical hyperphosphorylation of Akt at its two regulatory sites (Thr308 and Ser473). We explored whether inhibitor-induced hyperphosphorylation of A...