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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