<p>The <i>k</i><sub>inact</sub> and <i>K</i><sub>I</sub> values for the covalent inhibitors were obtained as described in the Experimental Procedures. The IC<sub>50</sub> values were calculated after 2 hours preincubation of the enzyme and inhibitor before addition of the substrate. Values are averages ± SD of three independent experiments.</p
<p><sup>*</sup>Values are means of at least three experiments. <sup>†</sup>Compounds were tested in ...
A novel rate equation is derived to characterize the dose-response behavior of a moderately potent (...
Enzyme inhibition studies are conducted to characterize enzymes and to examine drug-drug interaction...
<p>hNAAA was incubated with the compounds AM6701 (squares), <i>N-</i>Cbz-serine β-lactone (circles),...
<p>Panel (A). Reversible inhibition of hNAAA by AM9023. Panel (B). Irreversible inhibition of hNAAA ...
<p>Bars indicate the difference between the percentage inhibition observed using 0.11 mM GAL as subs...
[a]<p>The measurements were performed using 1 mM L-aspartate, 3 µM ADC, and 1 mM compound (potential...
<p>The concentration of the inhibitor was kept at 100 µM and the readings were taken under two subst...
[a]Assays were performed in duplicate (errors were less than 5%) with CENTA as reporter substrate (1...
<p>(A) Activity of HCHT on MU-NAG<sub>2</sub> substrate as a function of substrate concentration. (B...
Covalent inhibition has become more accepted in the past two decades, as illustrated by the clinical...
<p>Percentage residual activity was determined at various inhibitor concentrations using the followi...
<p>(<b>A</b>) Inhibition potencies of the candidate compounds. The magnitudes of inhibition by compo...
A difficulty associated with high throughput screening for enzyme inhibitors is to establish reactio...
A difficulty associated with high throughput screening for enzyme inhibitors is to establish reactio...
<p><sup>*</sup>Values are means of at least three experiments. <sup>†</sup>Compounds were tested in ...
A novel rate equation is derived to characterize the dose-response behavior of a moderately potent (...
Enzyme inhibition studies are conducted to characterize enzymes and to examine drug-drug interaction...
<p>hNAAA was incubated with the compounds AM6701 (squares), <i>N-</i>Cbz-serine β-lactone (circles),...
<p>Panel (A). Reversible inhibition of hNAAA by AM9023. Panel (B). Irreversible inhibition of hNAAA ...
<p>Bars indicate the difference between the percentage inhibition observed using 0.11 mM GAL as subs...
[a]<p>The measurements were performed using 1 mM L-aspartate, 3 µM ADC, and 1 mM compound (potential...
<p>The concentration of the inhibitor was kept at 100 µM and the readings were taken under two subst...
[a]Assays were performed in duplicate (errors were less than 5%) with CENTA as reporter substrate (1...
<p>(A) Activity of HCHT on MU-NAG<sub>2</sub> substrate as a function of substrate concentration. (B...
Covalent inhibition has become more accepted in the past two decades, as illustrated by the clinical...
<p>Percentage residual activity was determined at various inhibitor concentrations using the followi...
<p>(<b>A</b>) Inhibition potencies of the candidate compounds. The magnitudes of inhibition by compo...
A difficulty associated with high throughput screening for enzyme inhibitors is to establish reactio...
A difficulty associated with high throughput screening for enzyme inhibitors is to establish reactio...
<p><sup>*</sup>Values are means of at least three experiments. <sup>†</sup>Compounds were tested in ...
A novel rate equation is derived to characterize the dose-response behavior of a moderately potent (...
Enzyme inhibition studies are conducted to characterize enzymes and to examine drug-drug interaction...