Table 1:
Binding affinity of the tested PTH1R ligands
| Total Charges | KD (nM) | KD (0 mM) / KD (15 mM) | ||
|---|---|---|---|---|
|
| ||||
| Peptide | + / − (net charge) | 0 mM Ca2+ | 15 mM Ca2+ | |
|
| ||||
| PTH(1–34) | 7 / 4 (+3) | 1001 ± 41 | 204 ± 17** | 4.9 ± 0.5 |
| PTHrP(1–36) | 10 / 5 (+5) | 568 ± 37 | 495 ± 31 * | 1.1 ± 0.1 |
| PTH(1–34)E19AE22A | 7 / 2 (+5) | 224 ± 18 | 82 ± 6 ** | 2.7 ± 0.3 |
| PTH(1–14)PTHrP(15–36) | 9/4(+4) | 114 ± 5 | 76 ± 4 | 1.5 ± 0.1 |
| PTHrP(1–14)PTH(15–34) | 9 / 5(+4) | No binding | No binding | NA |
p<0.05 and
p<0.001 indicate significant difference in the fitted KD values for the tested ligand in the presence and absence of 15 mM Ca2+. The ratio KD(0 mM)/KD(15 mM) for PTH(1–34) is significantly different from the same ratio for all of the other tested ligands p < 0.0001.