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. 2009 Jul 28;284(39):26999–27009. doi: 10.1074/jbc.M109.028589

TABLE 1.

Inhibition kinetics of wild-type and mutant PfDHODH

The error represents the standard error of the mean for n = 4–5. The fold change is shown in parentheses. The IC50 values for A77 1726 against PfDHODH and hDHODH are 180 μm (19) and 0.3–1 μm (5456), respectively. Brequinar binds hDHODH with an IC50 of 0.006–0.01 μm (5456).

Inhibitor enzyme IC50
DSM1 DSM2 DSM74
μm
PfDHODH 0.047a 0.056a 0.28b
hDHODH >100a >100a >100b
PfDHODH-H185A 1.3 ± 0.17 (28) 1.3 ± 0.17 (23) 25 ± 9.0 (90)
PfDHODH-R265A 2.1 ± 0.70 (45) 2.4 ± 1.1 (43) 23 ± 6.7 (82)
PfDHODH-F227A 1.3 ± 0.086 (28) 4.4 ± 1.1 (79) 6.3 ± 1.1 (23)
PfDHODH-F188A 2.1 ± 1.4 (45) 0.21 ± 0.044 (4) 1.4 ± 0.37 (5)

a Data taken from Ref. 18.

b Data taken from Ref. 17.