Bias factors of AT1 receptor ligands modified at position 4
ΔΔLog(τ/KA) and BF values were calculated as described in Materials and Methods. Data are the mean ± S.E.M. of three to six independent experiments performed in triplicate.
| AngII | [Ile4]AngII | [Sar1Ile4]AngII | ||||
|---|---|---|---|---|---|---|
| ΔΔLog(τ/KA) | BF | ΔΔLog(τ/KA) | BF | ΔΔLog(τ/KA) | BF | |
| EGFR/Gq | 0.00 ± 0.12 | 1.00 | 1.13 ± 0.44 | 13.53 | 1.97 ± 0.26 | 92.69 |
| PKC/Gq | 0.00 ± 0.12 | 1.00 | 1.42 ± 0.48 | 26.24 | 1.76 ± 0.43 | 57.10 |
| βArrestin2/Gq | 0.00 ± 0.14 | 1.00 | 0.80 ± 0.43 | 6.36 | 1.12 ± 0.30 | 13.27 |
| βArrestin1/Gq | 0.00 ± 0.19 | 1.00 | 0.92 ± 0.44 | 8.23 | 1.08 ± 0.31 | 12.11 |
| G12/Gq | 0.00 ± 0.14 | 1.00 | 0.72 ± 0.47 | 5.29 | 0.98 ± 0.30 | 9.66 |
| EGFR/G12 | 0.00 ± 0.12 | 1.00 | 0.41 ± 0.27 | 2.56 | 0.98 ± 0.20 | 9.60 |
| EGFR/βarrestin1 | 0.00 ± 0.17 | 1.00 | 0.22 ± 0.19 | 1.64 | 0.88 ± 0.23 | 7.66 |
| EGFR/βarrestin2 | 0.00 ± 0.11 | 1.00 | 0.33 ± 0.17 | 2.13 | 0.84 ± 0.21 | 6.99 |
| PKC/G12 | 0.00 ± 0.12 | 1.00 | 0.70 ± 0.33 | 4.96 | 0.77 ± 0.40 | 5.91 |
| PKC/βarrestin1 | 0.00 ± 0.17 | 1.00 | 0.50 ± 0.28 | 3.19 | 0.67 ± 0.42 | 4.72 |
| PKC/βarrestin2 | 0.00 ± 0.11 | 1.00 | 0.62 ± 0.26 | 4.13 | 0.63 ± 0.41 | 4.30 |
| βArrestin2/G12 | 0.00 ± 0.14 | 1.00 | 0.08 ± 0.25 | 1.20 | 0.14 ± 0.26 | 1.37 |
| βArrestin1/G12 | 0.00 ± 0.19 | 1.00 | 0.19 ± 0.27 | 1.56 | 0.10 ± 0.27 | 1.25 |
| βArrestin1/βarrestin2 | 0.00 ± 0.19 | 1.00 | 0.11 ± 0.17 | 1.29 | −0.04 ± 0.28 | 0.91 |
| PKC/EGFR | 0.00 ± 0.09 | 1.00 | 0.29 ± 0.28 | 1.94 | −0.21 ± 0.38 | 0.62 |
BF, bias factor.