Table 1.

Kinetic parameters from recombinant PK-R enzymes measured with or without treatment with AG-348

EnzymeNo compound5 μM AG-348
Vmax, μmol/s/mgPEP KM, mMkcat, 1/skcat/KMVmax, μmol/s/mgPEP KM, mMkcat, 1/skcat/KM% of WT PK-R kcat/KM
WT0.691.1342.537.60.740.3245.7142.0378
R532W0.221.7313.67.90.210.4212.930.481
R510Q1.601.4598.868.11.640.32101.5317.3844
R479H0.501.6530.918.70.530.5532.458.5156
R486W0.341.4521.214.60.390.2524.298.4262
G332S0.142.738.33.00.151.119.48.523
R490W0.371.5222.815.00.390.5124.247.6127
G364D0.162.1410.14.70.220.5513.524.765
T384M0.111.426.94.80.120.377.219.351
  • kcat, first-order rate constant; kcat/KM, measure of enzymatic efficiency39; KM, substrate concentration to achieve half maximal velocity; Vmax, maximum velocity.