Figure 1: Exemestane (EXE), letrozole (LTZ) and anastrozole (ANA) selectively activate the human TRPA1 channel. | Nature Communications

Figure 1: Exemestane (EXE), letrozole (LTZ) and anastrozole (ANA) selectively activate the human TRPA1 channel.

From: Steroidal and non-steroidal third-generation aromatase inhibitors induce pain-like symptoms via TRPA1

Figure 1

(a) Representative traces of intracellular calcium response evoked by the aromatase inhibitors (AIs), EXE (100 μM), LTZ (100 μM) and ANA (100 μM), in HEK293 cells transfected with the cDNA for human TRPA1 (hTRPA1-HEK293), which respond to the selective TRPA1 agonist, allyl isothiocyanate (AITC; 30 μM). AITC (30 μM), EXE, LTZ and ANA (all 100 μM) fail to produce any calcium response in untransfected-HEK293 cells (HEK293). (b) Concentration-response curves to EXE, LTZ and ANA, yielded EC50 (95% confidence interval) of 58 (46–72) μM, 69 (43–109) μM, and 134 (96–186) μM, respectively. (c) AI-evoked calcium response in hTRPA1-HEK293 is abolished by the selective TRPA1 antagonist, HC-030031 (HC; 30 μM). (d) Representative traces of cells transfected with the cDNA codifying for the mutant hTRPA1 channel (3C/K-Q), which are insensitive to AITC (30 μM) or AIs (100 μM), but respond to the non-electrophilic agonist, menthol (100 μM), whereas HEK293 cells transfected with the cDNA codifying for wild-type hTRPA1 (WT) respond to all the drugs. Veh is the vehicle of AIs; dash (−) indicates the vehicle of HC. Each point or column represents the mean±s.e.m. of at least 25 cells from 3–6 independent experiments. §P<0.05 versus Veh, *P<0.05 versus EXE, LTZ or ANA group; ANOVA and Bonferroni post hoc test.

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