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Dear All,
We performed an experiment to determine the mechanism of inhibition of
ketoconazole (on 1-OH midazolam pathway) and ki values (human liver
microsmes). the mechanism of inhibiton of ketoconazole (0.001 uM -
0.1 uM) from our experiments is Non-competetive and the ki value is
0.0052 uM . We found in the literature that ketoconazole reported as
Competetive in some and Non- competetive also in some of the articles.
Can anybody explain this ?
Regards,
Raghav
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The following message was posted to: PharmPK
Raghav,
I believe the binding of ketoconazole is nonlinear with enzyme
concentration.
That said, the experimental design (i.e., series of varying inhibitor
concentrations, in a series of substrate concentrations, about a
series of
stable well-known enzyme concentrations) can reveal the noncompetitive
vs.
competitive or mixed ranges, if they exist.
Hope it helps.
-Shawn
Shawn D. Spencer, Ph.D., R.Ph.
Assistant Professor of Biopharmaceutics
Florida A&M College of Pharmacy
Tallahassee, FL 32307
shawn.spencer.aaa.famu.edu
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