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. Author manuscript; available in PMC: 2016 Jan 15.
Published in final edited form as: J Med Chem. 2015 Aug 28;58(17):6938–6959. doi: 10.1021/acs.jmedchem.5b00801

Figure 5.

Figure 5

FRα binding and PCFT uptake correlates with 4 and 7 growth inhibition toward IGROV1 and SKOV3 cells. Left panels: FRα levels were assayed by surface binding of [3H]folic acid (upper), whereas PCFT activity was measured with [3H]MTX (0.5 μM) over 5 min at 37 °C at pH 5.5 (lower). Right panels: Representative growth inhibition experiments for IGROV1 (upper) and SKOV3 (lower) cells treated with a range of concentrations of 4 or 7 in the absence (NA for no additions) or presence of 200 nM folic acid are shown. For both transport and binding assays, cell-associated radioactive substrate was expressed in units of pmol/mg protein. The methods are described in the Experimental Procedures.