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Table 1 Summary of pharmacological properties and basal level [3H]-D-Asp uptake

From: The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells

 

Substrate/Inhibitor

 

cell line

L-Glu (μM) IC50[pIC50 ± S.E.M.]

UCPH (μM) IC50[pIC50 ± S.E.M.]

TBOA (μM) IC50[pIC50 ± S.E.M.]

Basal Uptake [% of parental]

HCT116-PAR

21 [4.67 ± 0.04]

>100 [<4.0]

1.8 [5.75 ± 0.03]

100

HCT116-SN38

21 [4.67 ± 0.01]

>100 [<4.0]

1.5 [5.83 ± 0.08]

40 ± 1.8***

HCT116-Oxa

21 [4.67 ± 0.01]

>100 [<4.0]

1.5 [5.75 ± 0.08]

73 ± 6.9*

LoVo-PAR

26 [4.59 ± 0.04]

>100 [<4.0]

1.4 [5.84 ± 0.03]

100

LoVo-SN38

28 [4.54 ± 0.10]

>100 [<4.0]

1.9 [5.83 ± 0.11]

275 ± 35**

LoVo-Oxa

23 [4.64 ± 0.06]

>100 [<4.0]

2.7 [5.75 ± 0.03]

97 ± 8.0 NS

  1. IC50 values for the three compounds are in μM, with pIC50 values in brakets. The basal [3H]-D-Asp uptake data are based on the measured uptake in the chemotherapeutic-cells normalized to that in the relevant parental cell line on the experiment performed in duplicate. *) p <0.05,**) p <0.01,and ***) p <0.001, Compared to parental cell by two-tailed Student’s t-test