Table 1 TGFα shedding assay

From: Crystal structures of human ETB receptor provide mechanistic insight into receptor activation and partial activation

 

ETB (n = 7)

ETB-Y5 (n = 7)

ETA (n = 5)

Ligand

EC50, nM (pEC50 ± SEM)

Emax ± SEM, %

EC50, nM (pEC50 ± SEM)

Emax ± SEM, %

EC50, nM (pEC50 ± SEM)

Emax ± SEM, %

ET-1

0.11 (9.94 ± 0.04)

100

0.099 (10.01 ± 0.07)

100

0.13 (9.89 ± 0.04)

100

ET-3

0.13 (9.89 ± 0.04)

100.5 ± 0.6 (NS)

0.077 (10.12 ± 0.06)

100.9 ± 0.3 (NS)

0.65 (9.19 ± 0.03)

101.2 ± 0.8 (NS)

IRL1620

0.11 (9.97 ± 0.03)

87.6 ± 1.0***

0.92 (9.04 ± 0.04)

83.6 ± 1.4***

NA

NA

  1. The EC50 and Emax values of the AP-TGFα release response for the endothelin receptors. The Emax value of the AP-TGFα release response in the ET-1 treatment was normalized to 100% for each experiment. Emax values that significantly differ from the wild-type are denoted by asterisks
  2. *** P < 0.001 as compared with ET-1, one-way ANOVA with Dunnett’s post hoc test
  3. NS Not significant. NA Parameters not available owing to lack of responses
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