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Table 1 Characteristics of drugs and mean IC-50 values (± standard deviation)

From: Inhibition of tumour necrosis factor alpha production by activated T cells of rheumatoid arthritis patients by novel anti-folate drugs: an ex vivopilot study

     Mean IC-50 for TNF-α inhibition
Drug Target Reduced folate carrier affinity (cell uptake) Folylpolyglutamate synthetase affinity (cell retention) Rheumatoid arthritis patients (n = 11) Controls (n = 6)
MTX DHFR ++ + 78 (77) nM 57 (27) nM
PT523 DHFR +++ - 5.8 (3.2) nM 6.4 (8.3) nM
ZD1694 TS +++ +++ 16 (26) nM 4.8 (3.0) nM
SSZ NF-κB - - 278 (216) μM 191 (29) μM