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. 2019 Dec 4;28(2):677–689. doi: 10.1016/j.ymthe.2019.11.010

Table 2.

Hit Compounds Selected for Validation

ID Structure KM (PBG)a (μM) Vmaxa (nmol/min/mg)
Control – 86 ± 5 61 ± 2
C5 graphic file with name fx2.gif 81 ± 5 55 ± 1**
C6 graphic file with name fx3.gif 69 ± 4* 56 ± 1*
C11 graphic file with name fx4.gif 77 ± 5 59 ± 1
C17 graphic file with name fx5.gif 81 ± 2 58 ± 2

Chemical structure of the four hit compounds selected for cellular studies and steady-state enzyme kinetic parameters of HMBS in the presence of the compounds. *p < 0.05 and **p < 0.01 for significant difference compared with the values for the control sample (with 2% DMSO), calculated by unpaired two-tailed t test. Data are presented as mean ± SD.

a

Effect of the compounds on the enzyme kinetic parameters for HMBS activity, measured at fixed compound concentration (84 μM in 2% DMSO) and variable PBG (0–1 mM) at 37°C, and fitted to Michaelis-Menten kinetics.