Table 4.
Binding affinity of TAMRA-labelled fatty diacid acylated PYY analogues to human (HSA) and porcine (PSA) serum albumin.
| No. | Pos. | X-γGlu-2xAdo | HSA | PSA | ||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Kd (µM) pH 7.4 | pKd [95% CI] | Kd (µM) pH 6.0 | pKd [95% CI] | Kd (µM) pH 7.4 | pKd [95% CI] | Kd (µM) pH 6.0 | pKd[95% CI] | |||
| 53 | 7 | C18 diacid | 1.5 | 5.8 [5.9;5.7] | nd | nd | 1.7 | 5.8 [5.9;5.4] | nd | nd |
| 54 | 10 | C18 diacid | 0.83 | 6.1 [6.2;6.0] | nd | nd | 0.83 | 6.1 [6.2;6.0] | nd | nd |
| 55 | 25 | C18 diacid | 2.0 | 5.7 [5.7;5.7] | nd | nd | 2.2 | 5.7 [5.7;5.6] | nd | nd |
| 57 | 33 | C18 diacid | 0.76 | 6.1 [6.2;6.0] | nd | nd | 1.1 | 5.9 [6.1;5.8] | nd | nd |
| 58 | 30 | C14-diacid | 44 | 4.4 [4.5;4.3] | 23 | 4.6 [4.7;4.6] | 48 | 4.3 [4.4;4.3] | 34 | 4.5 [4.6;4.4] |
| 59 | 30 | C16-diacid | 4.2 | 5.4 [5.5;5.3] | 4.7 | 5.3 [5.5;5.2] | 4.5 | 5.4 [5.4;5.3] | 5.3 | 5.3 [5.4;5.2] |
| 56 | 30 | C18 diacid | 0.58 | 6.2 [6.3;6.2] | 0.93 | 6.0 [6.2;5.9] | 0.60 | 6.2 [6.3;6.1] | 0.89 | 6.1 [6.1;6.0] |
| 60 | 30 | C20-diacid | 0.098 | 7.0 [7.1;6.9] | 0.35 | 6.5 [6.7;6.2] | 0.27 | 6.6 [6.7;6.5] | 0.46 | 6.3 (6.6;6.1) |
| 61 | 30 | Acetyl | NB | – | – | – | NB | – | – | – |
pKd is calculated as the mean of three independent experiments, and the 95% confidence interval (CI) is given as [lower; upper]. The mean Kd in nM is calculated from the mean pKd.
X fatty diacid, NB no binding detected, nd not determined