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As stopped-flow analysis measures the overall change in protein fluorescence, and considering the kinetic allostery implied in the steady-state kinetics, it is possible to conclude that the rate limitation is related to structural changes
Steady state studies varying NADPH and inhibitor concentrations indicate that treatment with the fast inhibitors 7 and 8 or the slow inhibitor 3 , (the only slow inhibitor reaching equilibrium in 6 h), resulted in decreases in both K m and V max values consistent with uncompetitive inhibition of TGR, while treatment with 9 , a close analog of compound 8 synthesized ad hoc to facilitate structural studies (see below), changed only the V max indicating noncompetitive inhibition (Supplementary Tables 15 and 16)
A minority of patients experience minimal impulse-control gains
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