TABLE 7

Bias factors of AT1 receptor ligands modified at position 8

ΔΔLog(τ/KA) and BF values were calculated as described in the Materials and Methods. Data are the mean ± S.E.M. of three to six independent experiments performed in triplicate.

AngII[Ile8]AngII[Sar1Ile8]AngII[Ile8]AngIII
ΔΔLog(τ/KA)BFΔΔLog(τ/KA)BFΔΔLog(τ/KA)BFΔΔLog(τ/KA)BF
βArrestin2/PKC0.00 ± 0.111.003.19 ± 0.291547.83.35 ± 0.292252.11.54 ± 0.2334.88
βArrestin1/PKC0.00 ± 0.171.002.50 ± 0.43316.33.33 ± 0.432147.71.78 ± 0.2260.76
βArrestin2/EGFR0.00 ± 0.111.003.02 ± 0.311035.33.26 ± 0.241803.90.94 ± 0.288.74
βArrestin1/EGFR0.00 ± 0.171.002.33 ± 0.44211.613.24 ± 0.401720.31.18 ± 0.2715.22
G12/PKC0.00 ± 0.121.000.88 ± 0.507.622.19 ± 0.59155.000.81 ± 0.196.42
G12/EGFR0.00 ± 0.121.000.71 ± 0.515.102.09 ± 0.57124.160.21 ± 0.251.61
βArrestin2/G120.00 ± 0.141.002.31 ± 0.50203.131.16 ± 0.6114.530.74 ± 0.275.43
βArrestin1/G120.00 ± 0.191.001.62 ± 0.5941.521.14 ± 0.6913.860.98 ± 0.259.47
PKC/EGFR0.00 ± 0.091.000.17 ± 0.311.490.10 ± 0.181.250.60 ± 0.213.99
βArrestin2/βarrestin10.00 ± 0.191.00−0.69 ± 0.430.20−0.02 ± 0.50.950.24 ± 0.291.74
βArrestin1 /Gq0.00 ± 0.191.00NDNDNDNDNDND
βArrestin2/Gq0.00 ± 0.141.00NDNDNDNDNDND
G12/Gq0.00 ± 0.141.00NDNDNDNDNDND
PKC/Gq0.00 ± 0.121.00NDNDNDNDNDND
EGFR/Gq0.00 ± 0.121.00NDNDNDNDNDND
  • BF, bias factor; ND, cannot be determined.