Assays of cortisol-metabolizing enzymes in homogenates of human trabecular meshwork cells under optimal conditions revealed two defects in primary open-angle glaucoma (POAG): one is a marked increase in delta 4-reductase and the other is a decrease in 3-oxidoreductase. Experiments indicated that the differences in enzyme activities seen between POAG and nonPOAG trabecular meshwork derived cell ...

The synthesis of per-sulfated flavonoids, organic compounds with multiple sulfate groups, is challenging. We present here a two-step synthesis of fully sulfated flavonoids in high overall yields using the 2,2,2-trichloroethyl moiety as a protecting group. The two-step synthesis results in exclusive formation of the per-sulfated product in contrast to common sulfating agents that yield different...

Pregnane X receptor (PXR) regulates drug metabolism and is involved in drug-drug interactions. Prediction of PXR activators is important for evaluating drug metabolism and toxicity. Computational pharmacophore and quantitative structure-activity relationship models have been developed for predicting PXR activators. Because of the structural diversity of PXR activators, more efforts are needed f...

The heme-protein soluble guanylyl cyclase (sGC) is the intracellular receptor for nitric oxide (NO). sGC is a heterodimeric enzyme with α and β subunits and contains a heme moiety essential for binding of NO and activation of the enzyme. Stimulation of sGC mediates physiologic responses including smooth muscle relaxation, inhibition of inflammation, and thrombosis. In pathophysiologic states, N...

Optimal storage conditions to retain ribulose 1, 5-bisphosphate carboxylase/oxygenase (Rubisco) activity were investigated. The soluble spinach (Spinacia oleracea) enzyme was pretreated with its activators, Mg(2+) and HCO(3) (-), and then stored for up to 30 days at 4 or -18 degrees C or in liquid N(2). Cold inactivation and conformational changes were suggested to be involved during Rubisco st...

The effect of fatty acids with various structure and length in the hydrocarbon chain on the purified AMP deaminase from bovine brain was investigated. All the saturated fatty acids and unsaturated ones of trans configuration, longer than 16 in the hydrocarbon chain, were activators of the enzyme, while the unsaturated fatty acids of cis configuration including oleic, linoleic, linolenic, arachi...

teolytic enzyme plasmin (fibrinolysin) is supposed to be present in normal blood plasma in an inactive form, called plasminogen (proplasmin). Anxiety, strenuous exercise, hemorrhage, burn , t rauma (‘ ‘tourniquet shock’ ‘) and epinephrine admmistration have heels found to produce increased fibrinolytic activity (plasmin formation) in the blood. 3 The physiologic mechanism of activation of propl...