Specificity in enzyme inhibition. 1. Synthesis of 4-(4-imidazolyl)-3-amino-2-butanone, 4-(4-imidazolyl)-3-acetamido-2-butanone, and 4-(4-imidazolylmethyl 2,5-dimethyloxazole for assay as inhibitors of histidine decarboxylase

1971 ◽  
Vol 14 (10) ◽  
pp. 945-947 ◽  
Author(s):  
Edward E. Smissman ◽  
James A. Weis
Keyword(s):  
Enzyme Inhibition ◽  
Histidine Decarboxylase

Optimal Duration of the Preincubation Phase in Enzyme Inhibition Experiments

2020 ◽  
Author(s):  
Petr Kuzmic
Keyword(s):  
Enzyme Inhibition ◽  
Dose Response ◽  
Enzyme Inhibitor ◽  
Single Point ◽  
Association Rate ◽  
Weakly Bound ◽  
Inhibitor Complex ◽  
Dissociation Equilibrium ◽  
Optimal Duration ◽  
Algebraic Formula

This report describes an algebraic formula to calculate the optimal duration of the pre-incubation phase in enzyme-inhibition experiments, based on the assumed range of expected values for the dissociation equilibrium constant of the enzyme–inhibitor complex and for the bimolecular association rate constant. Three typical experimental scenarios are treated, namely, (1) single-point primary screening at relatively high inhibitor concentrations; (2) dose-response secondary screening of relatively weakly bound inhibitors; (3) dose-response screening of tightly-bound inhibitors.

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