Figure 3.
The inhibition mode of DAS734 on AtGPRAT2. (A) Inhibition kinetics showing that DAS734 is a competitive AtGPRAT2 inhibitor with respect to phosphoribosyl pyrophosphate (PRPP). The labels indicate different DAS734 concentrations. The data was fitted to the mixed inhibition model in GraphPad Prism software, and the alpha value of 12.56 calculated by this model indicated a competitive inhibition. Error bars are standard error of the mean (SEM) values of three independent experiments. (B) Structural superimposition of AtGPRAT2 with docked DAS734, EcGPRAT in the active [Protein Data Bank (PDB): 1ECC] and BsGPRAT in the inactive conformation (PDB: 1GPH). The cPRPP and 6-diazo-5-oxo-L-nor-leucine (DON) in the structure of 1ECC are shown as cyan sticks. The two AMP molecules in the A and C sites are shown as slate sticks. The docked DAS734 is shown in yellow sticks with the chlorine atom colored in gray.