Fitting of kinact and KI Values from Endpoint Pre-incubation IC50 Data
Lavleen K. Mader,
Jeffrey W. Keillor
Abstract:Experiments comprising a "pre-incubation" phase, where enzyme is incubated with inhibitor prior to the addition of assay substrate, are commonly used to evaluate covalent inhibitors, often via discontinuous or "endpoint" IC 50 assays. However, due to the lack of mathematical tools to describe its biphasic timedependent nature, this experiment has thus far been unable to provide k inact and K I values. Herein we report EPIC-Fit, a new method to determine k inact and K I values from global fitting of Endpoint Pr… Show more
Irreversible targeted covalent inhibitors, in the past regarded as inappropriately reactive and toxic, have seen a recent resurgence in clinical interest. This paradigm shift is attributed to the exploitation of...
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