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. Author manuscript; available in PMC: 2010 Nov 12.
Published in final edited form as: J Med Chem. 2009 Nov 12;52(21):6931–6935. doi: 10.1021/jm900823s

Figure 2. Phenoxy-herbicides and fibrates potently inhibit the human sweet-sensing receptor T1R2+T1R3.

Figure 2

T1R2+T1R3 subunits were transfected into HEK cells along with the promiscuous Gq-type protein G16-gust44. Activation of receptors by agonists was followed using the calcium-sensitive fluorescent dye fluo4-AM in a 96-well format with the fluorescent microplate reader Flexstation II (Molecular Devices). Inhibitors were added concomitantly with the sweetener sucralose at 2.5mM (saturating concentration).

A. Example of time-resolved raw traces of sucralose-activated T1R2+T1R3 receptor calcium response in the presence of increasing concentrations of the lactisole (10 to 100µM). Fluorescence signal (F) is expressed in arbitrary units (AU). The down arrow indicates the injection of the sweetener-inhibitors mixture on the cells. B,C. Dose-response curves showing inhibition of sucralose-activated human sweet receptor T1R2+T1R3 by phenoxy-herbicides and fibrates. Peak calcium signal is expressed as ΔF/F in %, normalized to control (sucralose alone). Data are from a representative experiment, means ± SD, done in quadruplicate.