Background: Myeloperoxidase (MPO), which is abundantly expressed in neutrophils, catalyzes the formation of a number of reactive oxidant species. However, evidence has emerged that MPO-derived oxidants contribute to tissue damage and initiation and propagation of inflammatory diseases, particularly, cardiovascular diseases. Therefore, studying the regulatory mechanisms of the enzyme activity is...

Accumulating evidence suggests that high expression of FGFR1 is closely related to the development of lung cancer especially in non-small cell lung cancers (NSCLC), to which non-ATP competitive inhibitors represent an effective therapeutical approach due to their good specificity. Herein, a series of NDGA analogues with the framework of bisaryl-1,4-dien-3-one as novel FGFR1 inhibitors have been...

Inhibition of recombinant D-amino acid oxidase from Trigonopsis variabilis (TvDAAO) activity in the presence of different sodium salts and potassium chloride is reported. A competitive inhibition pattern by sodium chloride was observed, and an inhibition constant value of K(i) = 85 mM was calculated. Direct connection of NaCl inhibition with FAD cofactor dissociation was confirmed by measuring ...

Addition of human cerebrospinal fluid (CSF) induced a marked inhibition of 3H-paroxetine binding to the monkey cortical membranes, while the specific binding of 3H-imipramine was slightly inhibited. Moreover, 3H-serotonin (5-hydroxy-tryptamine, 5-HT) uptake inhibition in the monkey cortical synaptosomes was also increased as the volume of added CSF was increased. Scatchard analysis of specific ...

Background: The aim of the present study was to investigate the in vitro effects of mercury (Hg+2), lead (Pb+2), silver (Ag+2), tin (Sn+2), bismuth (Bi+3) and indium (In+3) ions on sperm creatine kinase. Methods: creatine kinase was isolated from human sperm homogenates after chromatography on a DEAE cellulose column. Results: At 60 µg ml-1 metal concentration, 70% of the creatine kinase activi...

The inhibition of human erythrocyte glucose 6-phosphate dehydrogenase (G6PD) by Cd (II), Al (III) and Ni (II) was studied. The enzyme was partially purified having specific activity of 1.4 U/mg protein. Cadmium inhibited G6PD activity progressively up to 1.5 mM concentration where about 65% of the enzyme activity was lost. The inhibition was uncompetitive and noncompetitive with respect to gluc...

velocities in the forward and reverse directions was 54.5: 1 , somewhat lower than that previously reported (McQuate & Utter, 1959). Product-inhibition experiments with a non-saturating concentration of the constant substrate showed that in every case competitive inhibition occurs. This is consistent with a rapidequilibrium random Bi Bi mechanism for the reverse reaction, a similar mechanism to...

Initial velocity patterns for human placental choline acetyltransferase show a series of converging lines for both the forward and reverse reaction; with Kacetyl coenzyme A = 11.9 micron, Kcholine = 0.41 mM, KCOA = 8.8 micron, and Kacetylcholine = 1.3 mM. The relative rates of acetylcholine synthesis (Vf) to acetylcholine breakdown (Vr) is 4.5. Product inhibition by acetylcholine is competitive...

Topographically organized neurons represent multiple stimuli within complex visual scenes and compete for subsequent processing in higher visual centers. The underlying neural mechanisms of this process have long been elusive. We investigate an experimentally constrained model of a midbrain structure: the optic tectum and the reciprocally connected nucleus isthmi. We show that a recurrent antit...

K(+) is a competitive inhibitor of the uptake of the other alkali metal cations by yeast. Rb(+) is a competitive inhibitor of K(+) uptake, but Li(+), Na(+), and Cs(+) act like H(+). At relatively low concentrations they behave as apparent noncompetitive inhibitors of K(+) transport, but the inhibition is incomplete. At higher concentrations they inhibit the remaining K(+) transport competitivel...