The inhibition mechanisms of the firefly luciferase (Luc) by the two major products of the reactions catalysed by Luc, oxyluciferin and dehydroluciferyl-adenylate (L-AMP), were investigated. Light production in the presence and absence of these inhibitors (0.5 to 2 microM oxyluciferin; 0.0025 to 1.25 microM L-AMP) has been measured in 50 mM Hepes buffer (pH=7.5), 10 nM Luc, 250 microM ATP and D...

Initial rate studies were carried out using solubilized bovine brain hexokinase. Both ATP 4and 0i, y-5'-adenylyl methylene diphosphonate are competitive inhibitors of MgATP 2and mixed inhibitors of the sugar substrate, while N-acetylglucosamine, a competitive inhibitor of fructose, is a mixed inhibitor of MgATP 2. These results are consistent with a random Bi Bi mechanism for the brain enzyme. ...

A series of quinazolin-4(3H)-one derivatives were synthesised and evaluated for their cytotoxicity against human Caucasian breast adenocarcinoma (MCF-7) ovarian carcinoma (A2780) cell lines. Cytotoxicity the most tested compounds was 2- to 30-fold more than positive control lapatinib (IC50 2j = 3.79 ± 0.96; 3j 0.20 0.02; 5.9 0.74) MCF7 lines except two 2 b 15.72 0.07 2e 14.88 0.99). On other ha...

WS1358A1, a novel inhibitor of renal dehydropeptidase (DHP), augmented the urinary recovery of a carbapenem antibiotic imipenem and improved its protective effect in experimental infections when simultaneously administered to mice with the antibiotic. WS1358A1 was a competitive DHP inhibitor with a Ki value of 1.6 x 10(-7) M.

Rapamycin is widely used as a complete inhibitor of the mTORC1 nutrient-sensitive signaling complex. Using a novel ATP-competitive inhibitor named Torin1, we have found that many mTORC1 functions that regulate cap-dependent translation and autophagy are resistant to inhibition by rapamycin.